Ketoconazole is a synthetic antifungal medication that was first synthesized in the 1970s. It is used to treat a variety of fungal infections, including skin infections, vaginal yeast infections, and systemic infections. Ketoconazole works by inhibiting the synthesis of ergosterol, a vital component of fungal cell membranes. This disruption of ergosterol production leads to the death of fungal cells. Ketoconazole is well-absorbed after oral administration and is widely distributed throughout the body. It is metabolized in the liver and excreted in the urine and feces. The drug has been shown to have various effects on the human body, including its antifungal activity, anti-inflammatory properties, and effects on the immune system. Due to its broad spectrum of activity and its ability to penetrate into various tissues, ketoconazole is frequently used to treat a variety of fungal infections. It is also studied for its potential use in treating other conditions, such as cancer, autoimmune diseases, and viral infections. The study of ketoconazole continues to be of interest due to its potential therapeutic applications, its unique mechanism of action, and its ability to overcome drug resistance in some fungal infections.'
(2R,4S)-ketoconazole : A cis-1-acetyl-4-(4-{[2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy}phenyl)piperazine which dioxolane moiety has (2R,4S)-configuration. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]
1-acetyl-4-(4-{[2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy}phenyl)piperazine : A dioxolane that is 1,3-dioxolane which is substituted at positions 2, 2, and 4 by imidazol-1-ylmethyl, 2,4-dichlorophenyl, and [para-(4-acetylpiperazin-1-yl)phenoxy]methyl groups, respectively. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]
| ID Source | ID |
|---|---|
| PubMed CID | 456201 |
| CHEMBL ID | 75 |
| CHEBI ID | 48336 |
| SCHEMBL ID | 8407 |
| MeSH ID | M0011987 |
| PubMed CID | 3823 |
| CHEMBL ID | 157101 |
| CHEBI ID | 48339 |
| SCHEMBL ID | 8408 |
| SCHEMBL ID | 18258319 |
| MeSH ID | M0011987 |
| Synonym |
|---|
| AC-15957 |
| BIDD:GT0696 |
| MLS001146934 , |
| BRD-K29113274-001-03-6 |
| MLS000069784 , |
| smr000058460 |
| BPBIO1_000635 |
| EU-0100666 |
| ketoconazole, >=98% (hplc) |
| PRESTWICK_744 |
| tocris-1103 |
| NCGC00016907-01 |
| 1-[4-(4-{[(2r,4s)-2-(2,4-dichlorophenyl)-2-(1h-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy}phenyl)piperazin-1-yl]ethan-1-one |
| NCGC00025000-01 |
| chembl75 , |
| bdbm8610 |
| ketoconazole (k) |
| 24f2-1,25(oh)d3 |
| cas-65277-42-1 |
| LOPAC0_000666 |
| BSPBIO_000577 |
| 1-[4-[4-[[(2r,4s)-2-(2,4-dichlorophenyl)-2-(imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]piperazin-1-yl]ethanone |
| kz |
| ktz , |
| piperazine, (+/-)-1-acetyl-4-[4-[[(2r,4s)-2-(2,4-dichlorophenyl)-2-(1h-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]-, rel- |
| PRESTWICK3_000389 |
| (+)-ketoconazole |
| piperazine, (+)-1-acetyl-4-[4-[[2-(2,4-dichlorophenyl)-2-(1h-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]- |
| UPCMLD-DP138:001 |
| BIM-0050645.0001 |
| MLS000758224 |
| cpd000058460 , |
| UPCMLD-DP138 |
| PRESTWICK2_000389 |
| NCGC00025000-05 |
| NCGC00025000-03 |
| PRESTWICK1_000389 |
| PRESTWICK0_000389 |
| SPBIO_002498 |
| NCGC00025000-04 |
| NCGC00025000-07 |
| NCGC00025000-02 |
| NCGC00025000-06 |
| (2r,4s)-1-acetyl-4-(4-{[2-(2,4-dichlorophenyl)-2-(1h-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy}phenyl)piperazine |
| (2r,4s)-ketoconazole |
| 1-acetyl-4-(4-{[(2r,4s)-2-(2,4-dichlorophenyl)-2-(1h-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy}phenyl)piperazine |
| CHEBI:48336 , |
| NCGC00025000-08 |
| K 1003 , |
| dichlorophenyl)-2-(1h-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]-piperazine |
| HMS2089N05 |
| cis-1-acetyl-4-[4-[[2-(2,4- |
| HMS2051A19 |
| K0045 |
| (+/-)-cis-1-acetyl-4-[4-[[2-(2,4-dichlorophenyl)-2-(imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]piperazine |
| NCGC00025000-09 |
| MLS002207053 |
| MLS002222255 |
| rac-trans-ketoconazole |
| HMS1569M19 |
| NCGC00025000-10 |
| HMS2096M19 |
| HMS3262E13 |
| AKOS007930650 |
| ketocanazole |
| NCGC00253967-01 |
| tox21_300267 |
| MLS001423987 |
| tox21_110676 |
| dtxsid7029879 , |
| dtxcid301437106 |
| HMS2234H17 |
| 142128-59-4 |
| CCG-100815 |
| sr-01000597381 |
| SR-01000597381-6 |
| kuric |
| LP00666 |
| S1353 |
| EI-107 |
| CS-1846 |
| HY-B0105A |
| NC00065 |
| SCHEMBL8407 |
| KS-1205 , |
| NCGC00261351-01 |
| tox21_500666 |
| 1-(4-(4-(((2r,4s)-2-((1h-imidazol-1-yl)methyl)-2-(2,4-dichlorophenyl)-1,3-dioxolan-4-yl)methoxy)phenyl)piperazin-1-yl)ethanone |
| cis-1-acetyl-4-[4-[[2-(2,4-dichlorophenyl)-2-(1h-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl] methoxy]phenyl]piperazine |
| ketoconazole, antibiotic for culture media use only |
| Q-201267 |
| ketoconazole, british pharmacopoeia (bp) reference standard |
| bdbm60666 |
| us9150527, ketoconazole |
| OPERA_ID_397 |
| mfcd00058579 |
| ( inverted exclamation marka)-ketoconazol |
| SR-01000597381-1 |
| sr-01000075626 |
| SR-01000075626-1 |
| ketoconazole, united states pharmacopeia (usp) reference standard |
| ketoconazole, european pharmacopoeia (ep) reference standard |
| ketoconazole, pharmaceutical secondary standard; certified reference material |
| ketoconazole 2.0 mg/ml in methanol |
| SR-01000075626-4 |
| MRF-0000100 |
| HMS3713M19 |
| 1-(4-(4-(((2r,4s)-2-((1h-imidazol-1-yl)methyl)-2-(2,4-dichlorophenyl)-1,3-dioxolan-4-yl)methoxy)phenyl)piperazin-1-yl)ethan-1-one |
| SW196888-4 |
| HMS3678J17 |
| ketoconazole,(s) |
| Q27121163 |
| ketoconazole 100 microg/ml in acetonitrile |
| HMS3414J19 |
| BRD-K29113274-001-11-9 |
| BRD-K29113274-001-21-8 |
| SDCCGSBI-0050645.P002 |
| BCP28528 |
| NCGC00025000-28 |
| AMY917 |
| (+)-ketoconazol |
| (+)-r 41400 |
| NCGC00025000-14 |
| F84985 |
| NCGC00025000-16 |
| DTXSID901316748 |
| EN300-71972 |
| 1-[4-(4-{[(2r,4s)-2-(2,4-dichlorophenyl)-2-[(1h-imidazol-1-yl)methyl]-1,3-dioxolan-4-yl]methoxy}phenyl)piperazin-1-yl]ethan-1-one |
| 3-dioxolan-4-yl)-methoxy]phenyl)piperazine |
| M02048 |
| ethanone, 1-[4-[4-[[(2r,4s)-2-(2,4-dichlorophenyl)-2-(1h-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]-1-piperazinyl]- |
| HMS3267K04 |
| BRD-A76019558-001-01-0 |
| gtpl2568 |
| NCI60_002728 |
| r-41400 |
| xolegel |
| nsc-317629 |
| kw 1414 |
| KETOCONAZOLE , |
| nsc317629 |
| OPREA1_683648 |
| nsc 317629 |
| 79156-75-5 |
| DB01026 |
| 1-acetyl-4-(4-{[2-(2,4-dichlorophenyl)-2-(1h-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy}phenyl)piperazine |
| CHEBI:48339 , |
| FT-0656627 |
| 1-[4-[4-[[2-(2,4-dichlorophenyl)-2-(imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]piperazin-1-yl]ethanone |
| fungarest;fungoral |
| A19432 |
| CHEMBL157101 |
| AKOS015918262 |
| FT-0670621 |
| FT-0627575 |
| piperazine, (+/-)-1-acetyl-4-(4-(((2r,4s)-2-(2,4-dichlorophenyl)-2-(1h-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl)methoxy)phenyl)-, rel- |
| bdbm151585 |
| us8987315, ketoconazole |
| SCHEMBL8408 |
| 1-[4-(4-{[2-(2,4-dichlorophenyl)-2-(1h-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy}phenyl)piperazin-1-yl]ethanone |
| STL481884 |
| DTXSID20273956 |
| SCHEMBL18258319 |
| 1-acetyl-4-[4-[[2-(2,4-dichlorophenyl)-2-(1h-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]-methoxy] phenyl]piperazine |
| Q407883 |
| 1-(4-(4-((2-((1h-imidazol-1-yl)methyl)-2-(2,4-dichlorophenyl)-1,3-dioxolan-4-yl)methoxy)phenyl)piperazin-1-yl)ethanone |
| A911012 |
| EN300-297716 |
| 1-[4-(4-{[2-(2,4-dichlorophenyl)-2-[(1h-imidazol-1-yl)methyl]-1,3-dioxolan-4-yl]methoxy}phenyl)piperazin-1-yl]ethan-1-one |
Ketoconazole is a strong inhibitor of cytochrome P450 3A4 (CYP3A4) and of P-glycoprotein (P-gp) It is often used as an index inhibitor especially for CYP3a4-mediated drug metabolism. Its bioavailability and therapeutic efficacy are reduced by the low aqueous solubility of the drug.
Ketoconazole has been widely used as a strong cytochrome P450 (CYP) 3A (Cyp3A) inhibitor in drug-drug interaction (DDI) studies. The drug has been used worldwide for more than 30 years in CD, but in the absence of a large-scale study, its efficacy and tolerance are still under debate.
Ketoconazole is known to inhibit not only CYP3A but also CYP4F2. It was an inhibitor of fingolimod metabolism in HLM with an inhibition constant (K(i) of 0.74 μM. It did not produce any change in rosuvastatin pharmacokinetics in healthy subjects.
Treatment with ketoconazole (10 mg kg-1 daily) resulted in improvement in the first cat but unfortunately this animal was subsequently lost to follow-up. Treatment reduced Malassezia and increased fungal diversity to restore skin microbial communities.
The highest number of adverse events occurred with voriconazole, followed by ketoconazole. 2 dropouts occurred due to adverse events following itraconazole administration. Ketoconazol, fluconazole and BDDA proved to be very toxic to L.
The ratios of least square means (90% CI) of pharmacokinetic parameters in the presence and absence of ketoconazole for SPP301 and its metabolite were C(max) (maximum plasma concentration) 1. The Cmax ofCG100649 with CG100649 only and with concurrent administration of CG 100649 + ketoconzole were similar (10.5%)
Ketoconazole is a potent CYP3A inhibitor in vivo. Study arm 1, 20 subjects received saquinavir/ritonavir treatment alone for 14 days. In study arm 2, subjects received gemigliptin on 2 separate occasions.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Cilofungin, a lipopeptide antifungal agent, was tested for in vitro activity alone and in combination with ketoconazole, itraconazole, flucytosine and amphotericin B against 102 clinical isolates of Candida species." | ( In vitro comparison of cilofungin alone and in combination with other antifungal agents against clinical isolates of Candida species. Cobbs, CG; Dismukes, WE; Lank, KM; Smith, KR, 1991) | 0.49 |
| "Rifampin, a potent inducer of the hepatic microsomal system, has been shown to cause clinically important interactions when combined with other drugs, including oral anticoagulants, oral contraceptives, digitoxin, methadone hydrochloride, sulfonylureas, and barbiturates." | ( Update on rifampin drug interactions. Baciewicz, AM; Bekemeyer, WB; Self, TH, 1987) | 0.27 |
| " Recent evidence that it depresses testosterone synthesis in humans prompted us to investigate the effects in rats of its administration alone or in combination with the gonadotropin releasing hormone superagonist analogue leuprolide." | ( Inhibition of testosterone production with ketoconazole alone and in combination with a gonadotropin releasing hormone analogue in the rat. English, HF; Levine, HB; Santen, RJ; Santner, SJ, 1986) | 0.53 |
| "Two recent antifungal agents, miconazole and ketoconazole, were combined with three tissue conditioners and tested in vitro for their effects on the growth of Candida albicans." | ( The effectiveness, in vitro, of miconazole and ketoconazole combined with tissue conditioners in inhibiting the growth of Candida albicans. Quinn, DM, 1985) | 0.79 |
| "A total of 440 fresh clinical isolates of yeasts from cancer patients were tested by an agar dilution technique against miconazole, miconazole nitrate, and ketoconazole individually and combined with 5 micrograms of rifampin per ml." | ( In vitro activities of miconazole, miconazole nitrate, and ketoconazole alone and combined with rifampin against Candida spp. and Torulopsis glabrata recovered from cancer patients. Moody, MR; Morris, MJ; Schimpff, SC; Young, VM, 1980) | 0.7 |
| "We compared the in vitro antifungal action of amphotericin B (AmB) used alone or in combination with a second polyene antibiotic or with miconazole or ketoconazole." | ( Antifungal action of amphotericin B in combination with other polyene or imidazole antibiotics. Brajtburg, J; Kobayashi, D; Kobayashi, GS; Medoff, G, 1982) | 0.46 |
| " Flucytosine combined with amphotericin B produced little or no reduction of the MICs at which 90% of the strains were inhibited compared with amphotericin B alone." | ( In vitro activities of amphotericin B in combination with four antifungal agents and rifampin against Aspergillus spp. Gerding, DN; Harris, C; Hughes, CE; Moody, JA; Peterson, LR, 1984) | 0.27 |
| "A phase II clinical trial was performed to assess the antitumor activity and toxicity of ketoconazole in combination with doxorubicin (Adriamycin; Adria Laboratories, Columbus, OH) in patients with androgen-independent prostate cancer (AI PCa)." | ( Phase II study of ketoconazole combined with weekly doxorubicin in patients with androgen-independent prostate cancer. Amato, R; Bui, C; Ellerhorst, J; Kilbourn, R; Logothetis, CJ; Sella, A; Zukiwski, AA, 1994) | 0.84 |
| "In MRC-5 cell cultures, the efficacy of the acyclic nucleoside ganciclovir (GCV) against human cytomegalovirus (CMV) was unaffected when combined with either amphotericin B (AMP B), ketoconazole (KCZ), dapsone (DAP), or trimethoprim/sulfamethoxazole (TMP/SMX)." | ( Efficacy of ganciclovir in combination with other antimicrobial agents against cytomegalovirus in vitro and in vivo. Fraser-Smith, EB; Freitas, VR; Matthews, TR, 1993) | 0.48 |
| "Ten expressed human CYPs and human liver microsomes were used in the experiments for the identification of enzymes responsible for zonisamide metabolism and for the prediction of drug-drug interactions of zonisamide metabolism in humans from in vitro data, respectively." | ( Prediction of drug-drug interactions of zonisamide metabolism in humans from in vitro data. Kitada, M; Kiuchi, M; Nakamura, H; Nakasa, H; Ohmori, S; Ono, S; Tsutsui, M, 1998) | 0.3 |
| "We demonstrated that: (1) zonisamide is metabolized by recombinant CYP3A4, CYP2C19 and CYP3A5, (2) the metabolism is inhibited to a variable extent by known CYP3A4/5 substrates and/or inhibitors in human liver microsomes, and (3) in vitro-in vivo predictive calculations suggest that several compounds demonstrating CYP3A4-affinity might cause in vivo drug-drug interactions with zonisamide." | ( Prediction of drug-drug interactions of zonisamide metabolism in humans from in vitro data. Kitada, M; Kiuchi, M; Nakamura, H; Nakasa, H; Ohmori, S; Ono, S; Tsutsui, M, 1998) | 0.3 |
| "The metabolism of valspodar (PSC 833; PSC), which is developed as a multidrug resistance-reversing agent, was investigated to assess the potential for drug-drug interactions and the pharmacological activity of major metabolites." | ( The multidrug resistance modulator valspodar (PSC 833) is metabolized by human cytochrome P450 3A. Implications for drug-drug interactions and pharmacological activity of the main metabolite. Cohen, D; Fischer, V; Hauck, C; Heitz, F; Rodríguez-Gascón, A; Tynes, R; Vickers, AE, 1998) | 0.3 |
| " We tested the growth inhibitory activity of ketoconazole combined with 1,25-dihydroxyvitamin D3 (calcitriol) and with the vitamin D analogue EB 1089 in a preclinical model of prostate cancer." | ( Preclinical activity of ketoconazole in combination with calcitriol or the vitamin D analogue EB 1089 in prostate cancer cells. Feldman, D; Hsu, JY; Peehl, DM; Seto, E, 2002) | 0.88 |
| "Clonal assays with primary cultures of human prostatic cancer cells were performed to test anti-proliferative effects of ketoconazole alone or in combination with calcitriol or EB 1089." | ( Preclinical activity of ketoconazole in combination with calcitriol or the vitamin D analogue EB 1089 in prostate cancer cells. Feldman, D; Hsu, JY; Peehl, DM; Seto, E, 2002) | 0.83 |
| "In vitro metabolism studies were conducted to assess drug-drug interactions between perospirone, an antipsychotic agent, and concomitantly administered drugs--biperiden, flunitrazepam, haloperidol, and diazepam--using human liver microsomes." | ( In vitro drug-drug interactions with perospirone and concomitantly administered drugs in human liver microsomes. Kanamaru, H; Komuro, S; Mizuno, Y; Shimakura, J; Tani, N, ) | 0.13 |
| " The drug-drug interaction responsible for CYP3A enzyme(s) inhibition was observed when midazolam and inhibitors were co-administrated orally." | ( Model for the drug-drug interaction responsible for CYP3A enzyme inhibition. I: evaluation of cynomolgus monkeys as surrogates for humans. Baba, T; Kanazu, T; Koike, M; Okamura, N; Yamaguchi, Y, 2004) | 0.32 |
| " It was shown that the drug-drug interaction that occurs in vitro is also observed in vivo after oral administration of midazolam." | ( Model for the drug-drug interaction responsible for CYP3A enzyme inhibition. II: establishment and evaluation of dexamethasone-pretreated female rats. Baba, T; Kanazu, T; Koike, M; Okamura, N; Yamaguchi, Y, 2004) | 0.32 |
| " growth and to evaluate the effects of Pelargonium graveolens oil and its main components citronellol and geraniol combined with ketoconazole against Trichophyton spp." | ( Antifungal effects of herbal essential oils alone and in combination with ketoconazole against Trichophyton spp. Lim, S; Shin, S, 2004) | 0.76 |
| "The anti-Candida effects of estragole combined with amphotericin B or ketoconazole, commonly used antifungal drugs for treatment of candidasis, were evaluated in this study." | ( Anti-Candida effects of estragole in combination with ketoconazole or amphotericin B. Pyun, MS; Shin, S, 2004) | 0.81 |
| " As ciproxifan and thioperamide are inhibitors of cytochrome P450 enzymes, responsible for metabolizing risperidone and haloperidol, the possibility that the augmentation of antipsychotics by imidazoles resulted from drug-drug interactions was tested." | ( Lack of cataleptogenic potentiation with non-imidazole H3 receptor antagonists reveals potential drug-drug interactions between imidazole-based H3 receptor antagonists and antipsychotic drugs. Ballard, ME; Cowart, M; Decker, MW; Esbenshade, TA; Faghih, R; Fox, GB; Hancock, AA; Pan, L; Roberts, S; Rueter, LE; Zhang, M, 2005) | 0.33 |
| "The purpose of this randomized, single blinded clinical trial was to evaluate cytologically and clinically the efficacy of oral cephalexin alone and its combination with terbinafine or ketoconazole for the treatment of Malassezia dermatitis in dogs." | ( Comparison of the clinical efficacy of oral terbinafine and ketoconazole combined with cephalexin in the treatment of Malassezia dermatitis in dogs--a pilot study. Harris, BL; Kunkle, G; Lopez, J; Marsella, R; Nicklin, CF; Rosales, MS, 2005) | 0.76 |
| "A technique using a fully automated on-line solid phase extraction (SPE) system (Symbiosis, Spark Holland) combined with liquid chromatography (LC)-mass spectrometry (MS/MS) has been investigated for fast bioanalytical method development, method validation and sample analysis using both conventional C18 and monolithic columns." | ( Development and application of a new on-line SPE system combined with LC-MS/MS detection for high throughput direct analysis of pharmaceutical compounds in plasma. Alnouti, Y; Bi, H; Gusev, AI; Kavetskaia, O; Srinivasan, K; Waddell, D, 2005) | 0.33 |
| "In the current study, to understand the characteristics of dexamethasone (DEX)-treated female rats as an animal model for drug-drug interactions, a double-cannulation method was applied and separately assessed for the intestinal and hepatic first-pass metabolism of midazolam." | ( Assessment of the hepatic and intestinal first-pass metabolism of midazolam in a CYP3A drug-drug interaction model rats. Baba, T; Kanazu, T; Koike, M; Okamura, N; Yamaguchi, Y, 2005) | 0.33 |
| "This article reviews the in vitro metabolic and the in vivo pharmacokinetic drug-drug interactions with antifungal drugs, including fluconazole, itraconazole, micafungin, miconazole, and voriconazole." | ( [Drug-drug interaction of antifungal drugs]. Niwa, T; Shiraga, T; Takagi, A, 2005) | 0.33 |
| "Regulatory interest is increasing for drug transporters generally and P-glycoprotein (Pgp) in particular, primarily in the area of drug-drug interactions." | ( Development, validation and utility of an in vitro technique for assessment of potential clinical drug-drug interactions involving P-glycoprotein. Keogh, JP; Kunta, JR, 2006) | 0.33 |
| "The authors studied a potential drug-drug interaction via findings from in vitro and in vivo studies, to assess whether the in vitro system was predictive of in vivo clinical pharmacokinetic outcomes." | ( Predictive power of an in vitro system to assess drug interactions of an antimuscarinic medication: a comparison of in vitro and in vivo drug-drug interaction studies of trospium chloride with digoxin. Fox, L; Harnett, M; Lasseter, K; Profy, A; Sabounjian, L; Sandage, B; Shipley, J, 2006) | 0.33 |
| "Ketoconazole has generally been used as a standard inhibitor for studying clinical pharmacokinetic drug-drug interactions (DDIs) of drugs that are primarily metabolized by CYP3A4/5." | ( A novel model for the prediction of drug-drug interactions in humans based on in vitro cytochrome p450 phenotypic data. Balani, SK; Gan, LS; Lu, C; Miwa, GT; Prakash, SR, 2007) | 1.78 |
| "In drug-drug interaction (DDI) research, a two drug interaction is usually predicted by individual drug pharmacokinetics (PK)." | ( Drug-drug interaction prediction: a Bayesian meta-analysis approach. Chin, R; Flockhart, DA; Hall, SD; Li, L; Lucksiri, A; Yu, M, 2007) | 0.34 |
| "An 84-year-old man was admitted to the hospital for severe rhabdomyolysis induced by drug-drug interactions between simvastatin and ketoconazole and he recovered completely." | ( A lesson for everyone in drug-drug interactions. Akram, K; Parker, M; Rao, S, 2007) | 0.54 |
| "8-fold] when administered with ketoconazole, relative to when administered alone." | ( Pharmacokinetics of cinacalcet hydrochloride when administered with ketoconazole. Harris, RZ; Padhi, D; Salfi, M; Sullivan, JT, 2007) | 0.86 |
| "Numerous retrospective analyses have shown the utility of in vitro systems for predicting potential drug-drug interactions (DDIs)." | ( Application of CYP3A4 in vitro data to predict clinical drug-drug interactions; predictions of compounds as objects of interaction. Cook, J; Darekar, A; Dickins, M; Fahmi, O; Griffiths, M; Guo, F; Hurst, S; Hyland, R; Obach, RS; Phipps, A; Plowchalk, DR; Youdim, KA; Zayed, A, 2008) | 0.35 |
| "Using a generic approach for all test compounds, the findings from the current study showed the use of recombinant P450s provide a more robust in vitro measure of P450 contribution (fraction metabolized, f(m)) than that achieved when using chemical inhibitors in combination with human liver microsomes, for the prediction of potential CYP3A4 drug-drug interactions prior to clinical investigation." | ( Application of CYP3A4 in vitro data to predict clinical drug-drug interactions; predictions of compounds as objects of interaction. Cook, J; Darekar, A; Dickins, M; Fahmi, O; Griffiths, M; Guo, F; Hurst, S; Hyland, R; Obach, RS; Phipps, A; Plowchalk, DR; Youdim, KA; Zayed, A, 2008) | 0.35 |
| " Two approaches were used to determine fraction metabolized (f(m)); 1) by measuring substrate loss in human liver microsomes (HLM) in the presence and absence of specific chemical inhibitors and 2) by measuring substrate loss in individual cDNA expressed P450s (also referred to as recombinant P450s (rhCYP)) The fractions metabolized via each CYP were used to predict the drug-drug interaction due to CYP3A4 inhibition by ketoconazole using the modelling and simulation software SIMCYP." | ( Application of CYP3A4 in vitro data to predict clinical drug-drug interactions; predictions of compounds as objects of interaction. Cook, J; Darekar, A; Dickins, M; Fahmi, O; Griffiths, M; Guo, F; Hurst, S; Hyland, R; Obach, RS; Phipps, A; Plowchalk, DR; Youdim, KA; Zayed, A, 2008) | 0.51 |
| " Collections of individual case safety reports (ICSRs) related to suspected ADR incidents in clinical practice have proven to be very useful in post-marketing surveillance for pairwise drug--ADR associations, but have yet to reach their full potential for drug-drug interaction surveillance." | ( A statistical methodology for drug-drug interaction surveillance. Bate, A; Edwards, IR; Norén, GN; Sundberg, R, 2008) | 0.35 |
| "Traditional cytochrome P450 (P450) based drug-drug interaction (DDI) predictions are based on the ratio of an inhibitor's physiological concentration [I] and its inhibition constant K(i)." | ( Prediction of pharmacokinetic drug-drug interactions using human hepatocyte suspension in plasma and cytochrome P450 phenotypic data. II. In vitro-in vivo correlation with ketoconazole. Balani, SK; Berg, C; Hatsis, P; Lee, FW; Lu, C, 2008) | 0.54 |
| "To characterize the cytochrome P450 enzyme(s) responsible for the N-dealkylation of maraviroc in vitro, and predict the extent of clinical drug-drug interactions (DDIs)." | ( Maraviroc: in vitro assessment of drug-drug interaction potential. Collins, C; Dickins, M; Hyland, R; Jones, B; Jones, H, 2008) | 0.35 |
| "A novel method for the prediction of drug-drug interaction has been established based on the in vitro metabolic stability in the "serum incubation method" using cryopreserved human hepatocytes suspended in 100% human serum." | ( A novel approach to the prediction of drug-drug interactions in humans based on the serum incubation method. Chiba, M; Ishii, Y; Shibata, Y; Takahashi, H, 2008) | 0.35 |
| "In drug-drug interaction (DDI) research, a two-drug interaction is usually predicted by individual drug pharmacokinetics (PK)." | ( A Bayesian meta-analysis on published sample mean and variance pharmacokinetic data with application to drug-drug interaction prediction. Hall, S; Kim, S; Li, L; Wang, Z; Yu, M, 2008) | 0.35 |
| " In study arm 1, 20 subjects received saquinavir/ritonavir treatment alone for 14 days, followed in combination with ketoconazole treatment for 14 days." | ( Drug-drug interaction study of ketoconazole and ritonavir-boosted saquinavir. Bour, F; Kaeser, B; Schmitt, C; Zandt, H; Zhang, X; Zwanziger, E, 2009) | 0.85 |
| " Overall, the chemotherapy combined with Sr-89 was well tolerated." | ( Bone-targeted therapy: phase II study of strontium-89 in combination with alternating weekly chemohormonal therapies for patients with advanced androgen-independent prostate cancer. Amato, RJ; Henary, H; Hernandez-McClain, J, 2008) | 0.35 |
| "The vitro antifungal activity of retigeric acid B (RAB), a pentacyclic triterpenoid from the lichen species Lobaria kurokawae, was evaluated alone and in combination with fluconazole, ketoconazole, and itraconazole against Candida albicans using checkerboard microdilution and time-killing tests." | ( In vitro activities of retigeric acid B alone and in combination with azole antifungal agents against Candida albicans. Cheng, A; Lou, H; Sun, L; Sun, S; Wu, X; Zhang, Y, 2009) | 0.54 |
| "Antifungal effects of iron chelators (lactoferrin, deferoxamine, deferiprone, and ciclopirox) were tested alone and in combination with antifungal drugs against Aspergillus fumigatus B5233 conidia." | ( Antifungal activities of natural and synthetic iron chelators alone and in combination with azole and polyene antibiotics against Aspergillus fumigatus. Cruz, AR; Gallin, JI; Huang, CY; Zarember, KA, 2009) | 0.35 |
| "To assess drug-drug interactions of fesoterodine with cytochrome P450 (CYP) 3A4 inhibitor (ketoconazole), inducer (rifampicin), and substrates (ethinylestradiol and levonorgestrel)." | ( Evaluation of drug-drug interactions with fesoterodine. Malhotra, B; Sachse, R; Wood, N, 2009) | 0.57 |
| " The aim of this study is to investigate the synergistic anticandidal effect of xanthorrhizol in combination with ketoconazole or amphotericin B against Candida albicans, Candida glabrata, Candida guilliermondii, Candida krusei, Candida parapsilosis, and Candida tropicalis." | ( Synergistic anticandidal activity of xanthorrhizol in combination with ketoconazole or amphotericin B. Hwang, JK; Lee, K; Lee, MS; Rukayadi, Y; Yong, D, 2009) | 0.8 |
| " Oral ketoconazole is much easier and safer therapy than intramuscular SSG in combination with intralesional SSG in the treatment of localized cutaneous leishmaniasis." | ( Intralesional sodium stibogluconate alone or its combination with either intramuscular sodium stibogluconate or oral ketoconazole in the treatment of localized cutaneous leishmaniasis: a comparative study. Anwar, AE; El-Sayed, M, 2010) | 1.05 |
| "A novel in vitro model was recently developed in our laboratories for the prediction of magnitude of clinical pharmacokinetic drug-drug interactions (DDIs), based on reversible hepatic cytochrome P450 (P450) inhibition." | ( Quantitative prediction and clinical observation of a CYP3A inhibitor-based drug-drug interactions with MLN3897, a potent C-C chemokine receptor-1 antagonist. Balani, SK; Ducray, PS; Lu, C; Prakash, SR; Qian, MG; von Moltke, LL, 2010) | 0.36 |
| " However, when allicin was used in combination with fluconazole or ketoconazole, the MICs were decreased in some isolates." | ( In vitro investigation of antifungal activity of allicin alone and in combination with azoles against Candida species. Aala, F; Alizadeh, F; Chong, PP; Khodavandi, A; Sekawi, Z, 2010) | 0.6 |
| " The aim of this study was to evaluate the effectiveness of cabergoline (at doses of up 3 mg/week), alone or combined with relatively low doses of ketoconazole (up to 400 mg/day), in 12 patients with CD unsuccessfully treated by transsphenoidal surgery." | ( Effectiveness of cabergoline in monotherapy and combined with ketoconazole in the management of Cushing's disease. Agra, R; Albuquerque, JL; Arahata, CM; Arruda, MJ; Azevedo, MF; Canadas, V; Montenegro, L; Moura E Silva, L; Naves, LA; Pontes, L; Vilar, L, 2010) | 0.8 |
| "A method of assessing the risk of drug-drug interaction (DDI) caused by mechanism-based inhibition (MBI) was developed for early-stage drug development using cytochrome P450 (CYP) 3A4 inhibition screening data." | ( Prediction of drug-drug interactions based on time-dependent inhibition from high throughput screening of cytochrome P450 3A4 inhibition. Aso, Y; Higashida, A; Ishigai, M; Kato, M; Mitsui, T; Nabuchi, Y; Sekiguchi, N; Takanashi, K, 2009) | 0.35 |
| "Model-based drug-drug interaction (DDI) is an important in-silico tool to assess the in vivo consequences of in vitro DDI." | ( Drug-drug interaction prediction assessment. Hall, SD; Kim, S; Li, L; Qin, Z; Sara, QK; Wang, Z; Zhou, J, 2009) | 0.35 |
| "Nowadays, evaluation of potential risk of metabolic drug-drug interactions (mDDIs) is of high importance within the pharmaceutical industry, in order to improve safety and reduce the attrition rate of new drugs." | ( Predictions of metabolic drug-drug interactions using physiologically based modelling: Two cytochrome P450 3A4 substrates coadministered with ketoconazole or verapamil. Blasco, H; Bouzom, F; Cazade, F; Chenel, M; Perdaems, N; Vinson, C; Whalley, S, 2010) | 0.56 |
| " Thus, in vitro-in vivo extrapolation approaches were used to identify potential drug-drug interactions arising from inhibition of COD glucuronidation in humans." | ( In vitro-in vivo extrapolation predicts drug-drug interactions arising from inhibition of codeine glucuronidation by dextropropoxyphene, fluconazole, ketoconazole, and methadone in humans. Elliot, DJ; Janchawee, B; Miners, JO; Raungrut, P; Somogyi, AA; Uchaipichat, V, 2010) | 0.56 |
| " In combination with an increased throughput (up to 300%) and a reduced animal use (up to 50%), the enhanced power of the differential approach improves the utility of the biorelevant in situ perfusion technique with mesenteric blood sampling to elucidate the intestinal interaction profile of drugs and drug candidates." | ( Validation of a differential in situ perfusion method with mesenteric blood sampling in rats for intestinal drug interaction profiling. Annaert, P; Augustijns, P; Brouwers, J; Mols, R, 2010) | 0.36 |
| "Applying a comedication (COMD) covariate to apparent clearance (CL(app) = CL/F) is a common practice when using population pharmacokinetics (PopPK) to study metabolism-based drug-drug interactions (DDI)." | ( Bioavailability considerations in evaluating drug-drug interactions using the population pharmacokinetic approach. Duan, JZ; Jackson, AJ; Zhao, P, 2011) | 0.37 |
| "Ketoconazole and rifampin are the most widely used compounds examined in recent drug-drug interaction (DDI) studies, and they have multiple roles in modulating drug metabolizing enzymes and transporters." | ( Inhibitory effects of ketoconazole and rifampin on OAT1 and OATP1B1 transport activities: considerations on drug-drug interactions. Ahn, SH; Bae, MA; Choi, MK; Choi, YL; Jin, QR; Song, IS, 2011) | 2.13 |
| "To evaluate the efficacy and safety of CP alone and combined with ketoconazole shampoo 2% (KC) in the treatment of moderate to severe scalp seborrhoeic dermatitis." | ( Efficacious and safe management of moderate to severe scalp seborrhoeic dermatitis using clobetasol propionate shampoo 0·05% combined with ketoconazole shampoo 2%: a randomized, controlled study. Faergemann, J; Kerrouche, N; Lee, JH; Nikkels, AF; Ortonne, JP; Ponce Olivera, RM; Reich, K; Sidou, F, 2011) | 0.81 |
| " Recently, a synergistic antifungal effect of KTZ combined with BBR has been revealed." | ( Drug-drug interactions between ketoconazole and berberine in rats: pharmacokinetic effects benefit pharmacodynamic synergism. Dai, R; He, P; Liu, A; Liu, Y; Zhang, L; Zhou, Y, 2012) | 0.66 |
| "The aim of this crossover human male volunteer study was to investigate the utility of microdosing in the investigation of drug-drug interactions." | ( Predicting drug candidate victims of drug-drug interactions, using microdosing. Croft, M; Keely, B; Lappin, G; Morris, I; Tann, L, 2012) | 0.38 |
| " The changes in pharmacokinetics mediated by ketoconazole and fluvoxamine were quantitatively consistent with previously reported, non-microdose, drug-drug interaction data from studies including the same compounds." | ( Predicting drug candidate victims of drug-drug interactions, using microdosing. Croft, M; Keely, B; Lappin, G; Morris, I; Tann, L, 2012) | 0.64 |
| "The initial data reported here demonstrate the utility of microdosing to investigate the risk of development drugs being victims of drug-drug interactions." | ( Predicting drug candidate victims of drug-drug interactions, using microdosing. Croft, M; Keely, B; Lappin, G; Morris, I; Tann, L, 2012) | 0.38 |
| "Inhibition of cytochrome P450-mediated drug metabolism by a concomitantly administered second drug is one of the major causes of drug-drug interactions in humans." | ( Drug-drug interactions and cooperative effects detected in electrochemically driven human cytochrome P450 3A4. Di Nardo, G; Ferrero, S; Gilardi, G; Sadeghi, SJ, 2012) | 0.38 |
| "In this open-label, 2-part, 3-treatment, 1-sequence, 2-period crossover drug-drug interaction study, 1 group of subjects received a single 50-mg oral dose of gemigliptin on 2 separate occasions-once as monotherapy and again after pretreatment with 400 mg of oral ketoconazole once daily for 7 days." | ( Effects of ketoconazole and rifampicin on the pharmacokinetics of gemigliptin, a dipeptidyl peptidase-IV inhibitor: a crossover drug-drug interaction study in healthy male Korean volunteers. Bae, KS; Choi, HY; Jin, SJ; Kim, MJ; Kim, YH; Lim, HS; Noh, YH; Sung, HR, 2012) | 0.95 |
| " These findings suggest that gemigliptin may require a dose adjustment when concurrently administered with drugs that alter CYP3A4 activity." | ( Effects of ketoconazole and rifampicin on the pharmacokinetics of gemigliptin, a dipeptidyl peptidase-IV inhibitor: a crossover drug-drug interaction study in healthy male Korean volunteers. Bae, KS; Choi, HY; Jin, SJ; Kim, MJ; Kim, YH; Lim, HS; Noh, YH; Sung, HR, 2012) | 0.77 |
| "The hepatic organic anion transporting polypeptides (OATPs) influence the pharmacokinetics of several drug classes and are involved in many clinical drug-drug interactions." | ( Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions. Artursson, P; Haglund, U; Karlgren, M; Kimoto, E; Lai, Y; Norinder, U; Vildhede, A; Wisniewski, JR, 2012) | 0.38 |
| "Three simultaneously conducted phase I studies in advanced cancer patients used an adaptive escalation design to find the dose of oral, weekly sirolimus alone or in combination with either ketoconazole or grapefruit juice that achieves similar blood concentrations as its intravenously administered and approved prodrug, temsirolimus." | ( Phase I studies of sirolimus alone or in combination with pharmacokinetic modulators in advanced cancer patients. Cohen, EE; Eaton, KN; Fleming, GF; Fox-Kay, K; Gajewski, TF; Hartford, C; House, L; Kocherginsky, M; Maitland, ML; Moshier, K; Nallari, A; Ramirez, J; Ratain, MJ; Undevia, SD; Wu, K; Zha, Y, 2012) | 0.57 |
| " When used in combination with pegylated interferon and ribavirin, telaprevir has demonstrated a substantial increase in sustained virological response compared with pegylated interferon and ribavirin used alone." | ( Telaprevir: pharmacokinetics and drug interactions. Beaumont, M; Garg, V; Kauffman, RS; van Heeswijk, RP, 2012) | 0.38 |
| " Due to the difference in the IC50 values for CYP3A4 and CYP3A5, nonconcordant expression of CYP3A4 and CYP3A5 protein can significantly affect the observed magnitude of CYP3A-mediated drug-drug interactions in humans." | ( Effect of CYP3A5 expression on the inhibition of CYP3A-catalyzed drug metabolism: impact on modeling CYP3A-mediated drug-drug interactions. Chang, SY; Grubb, MF; Isoherranen, N; Peng, CC; Rodrigues, AD; Shirasaka, Y; Thummel, KE, 2013) | 0.39 |
| " Three studies were designed to evaluate the potential drug-drug interaction of netupitant with palonosetron and of the fixed dose combination of netupitant and palonosetron, NEPA, with an inhibitor (ketoconazole), an inducer (rifampicin) and a substrate (oral contraceptives) of CYP3A4." | ( Effect of netupitant, a highly selective NK₁ receptor antagonist, on the pharmacokinetics of palonosetron and impact of the fixed dose combination of netupitant and palonosetron when coadministered with ketoconazole, rifampicin, and oral contraceptives. Calcagnile, S; Henriksson, A; Kammerer, KP; Lanzarotti, C; Rossi, G; Timmer, W, 2013) | 0.77 |
| " In study 2, 36 subjects received NEPA alone (day 1) and in combination with ketoconazole or rifampicin." | ( Effect of netupitant, a highly selective NK₁ receptor antagonist, on the pharmacokinetics of palonosetron and impact of the fixed dose combination of netupitant and palonosetron when coadministered with ketoconazole, rifampicin, and oral contraceptives. Calcagnile, S; Henriksson, A; Kammerer, KP; Lanzarotti, C; Rossi, G; Timmer, W, 2013) | 0.81 |
| " This study evaluated the CYP3A-mediated drug-drug interaction potential of brentuximab vedotin and the excretion of MMAE." | ( CYP3A-mediated drug-drug interaction potential and excretion of brentuximab vedotin, an antibody-drug conjugate, in patients with CD30-positive hematologic malignancies. Alley, SC; Chen, R; Cooper, M; Gopal, AK; Goy, A; Grove, LE; Han, TH; Lynch, CM; Matous, JV; O'Connor, OA; Ramchandren, R, 2013) | 0.39 |
| "The present study aims to determine if an in vivo rat model of drug-drug interaction (DDI) could be useful to discriminate a sensitive (buspirone) from a 'non-sensitive' (verapamil) CYP3A substrate, using ketoconazole and ritonavir as perpetrator drugs." | ( Assessment of CYP3A-mediated drug-drug interaction potential for victim drugs using an in vivo rat model. Bellavance, E; Bourg, S; Duan, J; Garneau, M; Ribadeneira, MD; Rioux, N, 2013) | 0.58 |
| "The identification and quantification of potential drug-drug interactions is important for avoiding or minimizing the interaction-induced adverse events associated with specific drug combinations." | ( Pharmacokinetic drug interactions involving vortioxetine (Lu AA21004), a multimodal antidepressant. Buchbjerg, JK; Chen, G; Højer, AM; Lee, R; Serenko, M; Zhao, Z, 2013) | 0.39 |
| " Here, we address the clinical relevance of CYP3A4-related drug-drug interactions with midostaurin as either a "victim" or "perpetrator." | ( Investigation into CYP3A4-mediated drug-drug interactions on midostaurin in healthy volunteers. Dutreix, C; Lorenzo, S; Munarini, F; Roesel, J; Wang, Y, 2013) | 0.39 |
| " Drug-drug interactions involving voclosporin and CYP3A substrates are not expected." | ( Cytochrome P450 3A and P-glycoprotein drug-drug interactions with voclosporin. Aspeslet, LJ; Foster, RT; Freitag, DG; Huizinga, RB; Larouche, R; Ling, SY; Mayo, PR, 2014) | 0.4 |
| "To evaluate potential drug-drug interactions with the atypical antipsychotic lurasidone." | ( Lurasidone drug-drug interaction studies: a comprehensive review. Chiu, YY; Ereshefsky, L; Loebel, A; Poola, N; Preskorn, SH, 2014) | 0.4 |
| " No dose adjustment for lurasidone is needed when administered with lithium or valproate." | ( Lurasidone drug-drug interaction studies: a comprehensive review. Chiu, YY; Ereshefsky, L; Loebel, A; Poola, N; Preskorn, SH, 2014) | 0.4 |
| " The aim of the current work was to develop a novel physiologically based pharmacokinetic (PBPK) model to quantitatively assess the magnitude of CYP3A4 mediated drug-drug interactions with alisporivir as the substrate or victim drug." | ( Physiologically based pharmacokinetic modeling for assessing the clinical drug-drug interaction of alisporivir. Alexander, N; Barve, A; Einolf, H; Gu, H; Hanna, I; He, H; Heimbach, T; Ke, J; Mangold, JB; Sunkara, G; Wang, L; Xia, B; Zhang, T, 2014) | 0.4 |
| " Little is known about pomalidomide's potential for drug-drug interactions (DDIs); as pomalidomide clearance includes hydrolysis and cytochrome P450 (CYP450)-mediated hydroxylation, possible DDIs via CYP450 and drug-transporter proteins were investigated in vitro and in a clinical study." | ( Pomalidomide: evaluation of cytochrome P450 and transporter-mediated drug-drug interaction potential in vitro and in healthy subjects. Assaf, M; Hoffmann, M; Kasserra, C; Kumar, G; Li, Y; Liu, L; Palmisano, M; Wang, X, 2015) | 0.42 |
| " Therefore, evaluating the drug-drug interaction (DDI) potential associated with MMAE is important in the clinical development of ADCs." | ( Physiologically based pharmacokinetic modeling as a tool to predict drug interactions for antibody-drug conjugates. Chen, Y; Girish, S; Hop, C; Jin, JY; Li, C; Lu, D; Mukadam, S; Samineni, D; Shen, BQ; Wong, H, 2015) | 0.42 |
| "Physiologically based pharmacokinetic modeling was applied to characterize the potential drug-drug interactions for ruxolitinib." | ( Predicting drug-drug interactions involving multiple mechanisms using physiologically based pharmacokinetic modeling: a case study with ruxolitinib. Fraczkiewicz, G; Shi, JG; Williams, WV; Yeleswaram, S, 2015) | 0.42 |
| " The results indicate that the ternary system of ME combination with HP-β-CD may be a promising approach for skin targeting delivery of KET." | ( Synergetic skin targeting effect of hydroxypropyl-β-cyclodextrin combined with microemulsion for ketoconazole. Che, J; Guo, P; Lin, Y; Pan, W; Shao, W; Wu, C; Wu, Z; Xu, Y; Zeng, W; Zhang, G, 2015) | 0.63 |
| " This study was carried out to identify the contribution percentage of CYP450 to icotinib and use the results to develop a physiologically based pharmacokinetic (PBPK) model, which can help to predict drug-drug interaction (DDI)." | ( Relative contributions of the major human CYP450 to the metabolism of icotinib and its implication in prediction of drug-drug interaction between icotinib and CYP3A4 inhibitors/inducers using physiologically based pharmacokinetic modeling. Chen, J; Hu, P; Jiang, J; Liu, D; Zhao, Q; Zheng, X, 2015) | 0.42 |
| " Tasimelteon is rapidly absorbed, with a mean absolute bioavailability of approximately 38%, and is extensively metabolized primarily by oxidation at multiple sites, mainly by cytochrome P450 (CYP) 1A2 and CYP3A4/5, as initially demonstrated by in vitro studies and confirmed by the results of clinical drug-drug interactions presented here." | ( Clinical assessment of drug-drug interactions of tasimelteon, a novel dual melatonin receptor agonist. Baroldi, P; Dressman, MA; Kramer, WG; Ogilvie, BW; Torres, R, 2015) | 0.42 |
| " Pharmacokinetic (PK) drug-drug interactions (DDIs) were evaluated clinically between cabozantinib and (1) a CYP3A inducer (rifampin) in healthy volunteers, (2) a CYP3A inhibitor (ketoconazole) in healthy volunteers, and (3) a CYP2C8 substrate (rosiglitazone) in patients with solid tumors." | ( Pharmacokinetic (PK) drug interaction studies of cabozantinib: Effect of CYP3A inducer rifampin and inhibitor ketoconazole on cabozantinib plasma PK and effect of cabozantinib on CYP2C8 probe substrate rosiglitazone plasma PK. Benrimoh, N; Engel, C; Holland, J; Lacy, S; Miles, D; Nguyen, L; O'Reilly, T, 2015) | 0.82 |
| "The regulatory prohibition of ketoconazole as a CYP3A index inhibitor in drug-drug interaction (DDI) studies has compelled consideration of alternative inhibitors." | ( Ritonavir is the best alternative to ketoconazole as an index inhibitor of cytochrome P450-3A in drug-drug interaction studies. Greenblatt, DJ; Harmatz, JS, 2015) | 0.98 |
| "Ketoconazole has been widely used as a strong cytochrome P450 (CYP) 3A (CYP3A) inhibitor in drug-drug interaction (DDI) studies." | ( Best practices for the use of itraconazole as a replacement for ketoconazole in drug-drug interaction studies. Bello, A; Dresser, MJ; Heald, D; Komjathy, SF; Liu, L; O'Mara, E; Robertson, SM; Rogge, M; Stoch, SA, 2016) | 2.12 |
| " Overall, the safety profile of romidepsin was not altered by coadministration with ketoconazole or rifampin, except that a higher incidence and greater severity of thrombocytopenia was observed when romidepsin was given with rifampin." | ( Evaluation of CYP3A-mediated drug-drug interactions with romidepsin in patients with advanced cancer. Arkenau, HT; Burris, HA; Infante, J; Jones, SF; Laille, E; Lemech, C; Liu, L; Patel, M, 2015) | 0.64 |
| " These predictions were in good agreement with clinical single dose drug-drug interaction studies, but not with reports of imatinib interactions at steady-state." | ( Human hepatocyte assessment of imatinib drug-drug interactions - complexities in clinical translation. Beumer, JH; Christner, SM; Kiesel, BF; Parise, RA; Pillai, VC; Rudek, MA; Venkataramanan, R, 2015) | 0.42 |
| " The main objectives of the present study were to: 1) develop and refine a physiologically based pharmacokinetic (PBPK) model of crizotinib on the basis of clinical single- and multiple-dose results, 2) verify the crizotinib PBPK model from crizotinib single-dose drug-drug interaction (DDI) results with multiple-dose coadministration of ketoconazole or rifampin, and 3) apply the crizotinib PBPK model to predict crizotinib multiple-dose DDI outcomes." | ( Prediction of Drug-Drug Interactions with Crizotinib as the CYP3A Substrate Using a Physiologically Based Pharmacokinetic Model. Johnson, TR; Smith, BJ; Yamazaki, S, 2015) | 0.59 |
| "The present study was conducted to investigate the influence of the strong CYP3A4 inhibitor ketoconazole (KTZ) on the pharmacokinetics of drospirenone (DRSP) administered in combination with ethinylestradiol (EE) or estradiol (E2)." | ( Pharmacokinetic interaction between the CYP3A4 inhibitor ketoconazole and the hormone drospirenone in combination with ethinylestradiol or estradiol. Berse, M; Gschwend, S; Höchel, J; Klein, S; Schütt, B; Wiesinger, H; Zollmann, FS, 2015) | 0.88 |
| "A moderate pharmacokinetic drug-drug interaction between DRSP and KTZ was demonstrated in this study." | ( Pharmacokinetic interaction between the CYP3A4 inhibitor ketoconazole and the hormone drospirenone in combination with ethinylestradiol or estradiol. Berse, M; Gschwend, S; Höchel, J; Klein, S; Schütt, B; Wiesinger, H; Zollmann, FS, 2015) | 0.66 |
| "Domperidone is a dopamine receptor antagonist and a substrate of CYP3A4, hence there is a potential for CYP3A inhibition-based drug-drug interactions (DDI)." | ( A physiologically based pharmacokinetic modeling approach to predict drug-drug interactions between domperidone and inhibitors of CYP3A4. Ravenstijn, P; Sensenhauser, C; Snoeys, J; Templeton, I, 2016) | 0.43 |
| "This example of the application of PBPK modeling to predict drug-drug interactions was used to support the labeling of macitentan (Opsumit)." | ( Physiologically-Based Pharmacokinetic Modeling of Macitentan: Prediction of Drug-Drug Interactions. Buchmann, S; de Kanter, R; Delahaye, S; Gnerre, C; Kohl, C; Segrestaa, J; Sidharta, PN; Treiber, A, 2016) | 0.43 |
| " The aim of the present study was to improve the dissolution rate and hence the oral bioavailability of a poorly water soluble imidazole antifungal model drug, ketoconazole (KET), via the preparation of SDs using phospholipid carriers either alone or in combination with other hydrophilic carriers." | ( Potential use of phospholipids in combination with hydrophilic carriers for enhancement of the dissolution and oral bioavailability of imidazole antifungal Class II drugs. Abu Hashim, II; El-Shabouri, MH; Ghazy, NF, 2015) | 0.61 |
| "Ketoconazole is a potent CYP3A inhibitor in vivo, and frequently serves as an index CYP3A inhibitor in drug-drug interaction (DDI) studies with healthy volunteers." | ( Ketoconazole-Associated Liver Injury in Drug-Drug Interaction Studies in Healthy Volunteers. Banankhah, PS; Garnick, KA; Greenblatt, DJ, 2016) | 3.32 |
| " Drug-drug interactions (DDIs) based on P-gp/CYP3A interplay are of clinical importance and require preclinical investigation." | ( The Consequence of Drug-Drug Interactions Influencing the Interplay between P-Glycoprotein and Cytochrome P450 3a: An Ex Vivo Study with Rat Precision-Cut Intestinal Slices. de Graaf, IA; de Jager, MH; Groothuis, GM; Li, M; Siissalo, S; van Dam, A, 2016) | 0.43 |
| " Study A: When given with ketoconazole, abiraterone exposure increased by 9% for maximum plasma concentration (Cmax ) and 15% for area under the plasma concentration-time curve from 0 to time of the last quantifiable concentration (AUClast ) and AUC from time 0 to infinity (AUC∞ ) compared to abiraterone acetate alone." | ( Impact on abiraterone pharmacokinetics and safety: Open-label drug-drug interaction studies with ketoconazole and rifampicin. Acharya, M; Bernard, A; Chien, C; De Vries, R; Jiao, J; Monbaliu, J; Stieltjes, H; Tran, N; Vaccaro, N; Yu, M, 2015) | 0.93 |
| " The FDA report advised against the use ketoconazole tablets as a first-line treatment for any fungal infections because of the risk of potentially serious drug-drug interactions and liver and adrenal gland complications." | ( No Increased Risk of Ketoconazole Toxicity in Drug-Drug Interaction Studies. Hohmann, N; Mikus, G; Outeiro, N, 2016) | 1.02 |
| " In order to identify the best inhibitor concentration for the accurate prediction of magnitude of a hepatic cytochrome P450 (CYP)-mediated drug-drug interaction (DDI), the DDI between nifedipine, the CYP substrate probe, and fluconazole, ketoconazole, or ritonavir, the CYP inhibitors, in in situ rat liver perfusion system and rats were investigated." | ( Unbound liver concentration is the true inhibitor concentration that determines cytochrome P450-mediated drug-drug interactions in rat liver. Amano, N; Funami, M; Hirabayashi, H; Iwasaki, S, 2017) | 0.64 |
| " Three edoxaban drug-drug interaction studies examined the effects of P-gp inhibitors with varying degrees of CYP3A4 inhibition." | ( Edoxaban drug-drug interactions with ketoconazole, erythromycin, and cyclosporine. Matsushima, N; Mendell, J; Parasrampuria, DA; Shi, M; Truitt, K; Zahir, H, 2016) | 0.71 |
| " The mean maximum QTcF increase from baseline was 407, 487, and 437 milliseconds for AZD1305, alone and in combination with verapamil or ketoconazole, respectively." | ( In Silico Predictions and In Vivo Results of Drug-Drug Interactions by Ketoconazole and Verapamil on AZD1305, a Combined Ion Channel Blocker and a Sensitive CYP3A4 Substrate. Aunes, M; Cullberg, M; Edvardsson, N; Frison, L; Johansson, S; Löfberg, B; Lunde, H, 2016) | 0.87 |
| "Intestinal P-gp and CYP3A4 work coordinately to reduce the intracellular concentration of drugs, and drug-drug interactions (DDIs) based on this interplay are of clinical importance and require pre-clinical investigation." | ( The consequence of regional gradients of P-gp and CYP3A4 for drug-drug interactions by P-gp inhibitors and the P-gp/CYP3A4 interplay in the human intestine ex vivo. de Graaf, IA; de Jager, MH; Groothuis, GM; Li, M; van de Steeg, E, 2017) | 0.46 |
| " The main objectives of this study were to 1) develop physiologically based pharmacokinetic (PBPK) models of bosutinib; 2) verify and refine the PBPK models based on clinical study results of bosutinib single-dose drug-drug interaction (DDI) with ketoconazole and rifampin, as well as single-dose drug-disease interaction (DDZI) in patients with renal and hepatic impairment; 3) apply the PBPK models to predict DDI outcomes in patients with weak and moderate CYP3A inhibitors; and 4) apply the PBPK models to predict DDZI outcomes in renally and hepatically impaired patients after multiple-dose administration." | ( Application of Physiologically Based Pharmacokinetic Modeling to the Understanding of Bosutinib Pharmacokinetics: Prediction of Drug-Drug and Drug-Disease Interactions. Abbas, R; Hsyu, PH; Loi, CM; Ono, C; Yamazaki, S, 2017) | 0.64 |
| " Patients undergoing hematopoietic stem cell transplantation (HSCT) are exposed to various types of drugs, and understanding how these drugs interact is of the utmost importance." | ( Development of an assay for cellular efflux of pharmaceutically active agents and its relevance to understanding drug interactions. Andersson, BS; Hassan, M; Valdez, BC, 2017) | 0.46 |
| " Eighty-eight patients were enrolled across the 3 drug-drug interaction studies; the ixazomib toxicity profile was consistent with previous studies." | ( Effects of Strong CYP3A Inhibition and Induction on the Pharmacokinetics of Ixazomib, an Oral Proteasome Inhibitor: Results of Drug-Drug Interaction Studies in Patients With Advanced Solid Tumors or Lymphoma and a Physiologically Based Pharmacokinetic Ana Bessudo, A; Esseltine, DL; Gupta, N; Hanley, MJ; Ke, A; Liu, G; Nemunaitis, J; O'Neil, BH; Patel, C; Rasco, DW; Rowland Yeo, K; Sharma, S; Venkatakrishnan, K; Wang, B; Xia, C; Zhang, X, 2018) | 0.48 |
| " A physiologically based pharmacokinetic (PBPK) model that includes inhibition constant evaluated in cryopreserved hepatocytes was used to predict drug-drug interactions (DDIs) between orally administered nifedipine, a CYP substrate, and fluconazole or ketoconazole, CYP inhibitors, in rats." | ( Quantitative prediction of the extent of drug-drug interaction using a physiologically based pharmacokinetic model that includes inhibition of drug metabolism determined in cryopreserved hepatocytes. Amano, N; Hirabayashi, H; Iwasaki, S, 2018) | 0.66 |
| " It has been demonstrated to be informative and helpful to quantify the modification in drug exposure due to specific physio-pathological conditions, age, genetic polymorphisms, ethnicity and particularly drug-drug interactions (DDIs)." | ( Prediction of drug-drug interactions using physiologically-based pharmacokinetic models of CYP450 modulators included in Simcyp software. Daali, Y; Desmeules, JA; Marsousi, N; Rudaz, S, 2018) | 0.48 |
| " The purpose of this research was to predict the magnitude of drug-drug interaction (DDI) after coadministration of a strong CYP3A4 inducer or inhibitor using physiologically based pharmacokinetic (PBPK) modeling." | ( A Physiologically Based Pharmacokinetic Modeling Approach to Predict Drug-Drug Interactions of Buprenorphine After Subcutaneous Administration of CAM2038 With Perpetrators of CYP3A4. Gobburu, JVS; Liu, T, 2018) | 0.48 |
| " In vitro and clinical drug-drug interaction (DDI) studies indicated that midostaurin and its metabolites are substrates, reversible and time-dependent inhibitors, and inducers of CYP3A4." | ( Simultaneous Physiologically Based Pharmacokinetic (PBPK) Modeling of Parent and Active Metabolites to Investigate Complex CYP3A4 Drug-Drug Interaction Potential: A Case Example of Midostaurin. Chun, DY; Dutreix, C; Einolf, HJ; Gu, H; He, H; Ouatas, T; Rebello, S; Wang, L, 2018) | 0.48 |
| " In vitro assessment of the proarrhythmic potential of drugs is limited to one compound and thus neglects the potential of drug-drug interactions, including those involving active metabolites." | ( Drug interaction at hERG channel: In vitro assessment of the electrophysiological consequences of drug combinations and comparison against theoretical models. Kulig, M; Lisowski, B; Polak, S; Wiśniowska, B, 2018) | 0.48 |
| " CC-223 was studied in vitro for metabolism and drug-drug interactions (DDI), and in clinic for interaction with ketoconazole." | ( Assessment of drug-drug interaction potential and PBPK modeling of CC-223, a potent inhibitor of the mammalian target of rapamycin kinase. Atsriku, C; Li, Y; Liu, H; Narayanan, R; Nissel, J; Surapaneni, S; Tong, Z; Wang, X, 2019) | 0.72 |
| " Hepatic clearance and drug-drug interactions (DDI) were estimated by in vitro in vivo extrapolation (IVIVE) based on parameters obtained from in vitro experiments." | ( Application of physiologically based pharmacokinetic modeling to the prediction of drug-drug and drug-disease interactions for rivaroxaban. Ge, W; Jiang, Q; Xu, R, 2018) | 0.48 |
| " Our primary objectives were to: 1) refine the previously developed bosutinib PBPK model on the basis of the latest oral bioavailability data and 2) verify the refined PBPK model with P-glycoprotein kinetics on the basis of the bosutinib drug-drug interaction (DDI) results with ketoconazole and rifampin." | ( Application of Physiologically Based Pharmacokinetic Modeling in Understanding Bosutinib Drug-Drug Interactions: Importance of Intestinal P-Glycoprotein. Costales, C; Kimoto, E; Loi, CM; Varma, MV; Yamazaki, S, 2018) | 0.66 |
| "The potential consequences of drug-drug interactions on the excretion profile of the anabolic androgenic steroid methandienone (17β-hydroxy-17α-methylandrosta-1,4-dien-3-one) are discussed." | ( Drug-drug interaction and doping: Effect of non-prohibited drugs on the urinary excretion profile of methandienone. Botrè, F; de la Torre, X; Fiacco, I; Khevenhüller-Metsch, FL; Mazzarino, M; Parr, MK, 2018) | 0.48 |
| " To evaluate drug-drug interactions, the impact of ketoconazole, a known strong inhibitor of cytochrome P450 3A4 and P-glycoprotein, was studied." | ( Microdosed Cocktail of Three Oral Factor Xa Inhibitors to Evaluate Drug-Drug Interactions with Potential Perpetrator Drugs. Burhenne, J; Foerster, KI; Haefeli, WE; Lehmann, ML; Mikus, G; Schaumaeker, M, 2019) | 0.77 |
| " This is the first study that has been conducted to evaluate drug-drug interactions with a drug class, and the low administered doses also allow evaluation in vulnerable target populations." | ( Microdosed Cocktail of Three Oral Factor Xa Inhibitors to Evaluate Drug-Drug Interactions with Potential Perpetrator Drugs. Burhenne, J; Foerster, KI; Haefeli, WE; Lehmann, ML; Mikus, G; Schaumaeker, M, 2019) | 0.51 |
| " Potential drug-drug interactions (DDIs) following coadministration of these 2 overactive bladder treatments were estimated using physiologically based pharmacokinetic models, developed and verified by comparing predicted and observed pharmacokinetic profiles from clinical studies." | ( Physiologically Based Pharmacokinetic Modeling Suggests Limited Drug-Drug Interaction for Fesoterodine When Coadministered With Mirabegron. Goosen, TC; Lin, J; Malhotra, B; Tse, S; Yamagami, H, 2019) | 0.51 |
| "We verified a physiologically-based pharmacokinetic (PBPK) model to predict cytochrome P450 3A4/5-mediated drug-drug interactions (DDIs)." | ( Quantitative Prediction of CYP3A4- and CYP3A5-Mediated Drug Interactions. Dickinson, GL; Guo, Y; Hall, SD; Hilligoss, JK; Lucksiri, A; Vuppalanchi, RK, 2020) | 0.56 |
| " Compared with the controls, ketoconazole combined with CNIs can significantly reduce the dose of CNIs in patients receiving solid organ transplantation (WMD = -203." | ( Efficacy and safety of ketoconazole combined with calmodulin inhibitor in solid organ transplantation: A systematic review and meta-analysis. Chen, C; Cui, Y; Li, M; Ma, L; Wu, S; Xue, T; Yang, T; Zhou, Y, 2020) | 1.16 |
| " Despite the extensive clinical use of bortezomib, the mechanism of the complex time-dependent pharmacokinetics of bortezomib has not been fully investigated in context of its pharmacodynamics (PD) and drug-drug interaction (DDI) profiles." | ( A Translational Physiologically Based Pharmacokinetics/Pharmacodynamics Framework of Target-Mediated Disposition, Target Inhibition and Drug-Drug Interactions of Bortezomib. Hanley, M; Iwasaki, S; Venkatakrishnan, K; Xia, C; Zhu, A, 2020) | 0.56 |
| "Numerous drug-drug interaction (DDI) trials have to be conducted in healthy volunteers based on current regulatory guidelines." | ( Proposal of a Safe and Effective Study Design for CYP3A-Mediated Drug-Drug Interactions. Mikus, G; Rohr, BS, 2020) | 0.56 |
| " This method was successfully applied to establish the cell pharmacokinetics methodology and preliminary studied the metabolism of drug-drug interaction of ketoconazole and dexamethasone acetate." | ( Simultaneous determination the concentration change of ketoconazole and dexamethasone acetate: application to drug-drug interaction in human keratinocyte. Li, H; Li, L; Ma, P; Qian, K; Wang, C, 2020) | 1 |
| "Develop a physiologically based pharmacokinetic (PBPK) model of ivosidenib using in vitro and clinical PK data from healthy participants (HPs), refine it with clinical data on ivosidenib co-administered with itraconazole, and develop a model for patients with acute myeloid leukemia (AML) and apply it to predict ivosidenib drug-drug interactions (DDI)." | ( Physiologically based pharmacokinetic modeling and simulation to predict drug-drug interactions of ivosidenib with CYP3A perpetrators in patients with acute myeloid leukemia. Fan, B; Ke, A; Le, K; Prakash, C; Yang, H, 2020) | 0.56 |
| " For the first time, we developed a physiologically based pharmacokinetic (PBPK) model-based approach to assess CYP3A-mediated drug-drug interaction (DDI) risk for polatuzumab vedotin (Polivy), an anti-CD79b-vc-monomethyl auristatin E (MMAE) antibody-drug conjugate (ADC)." | ( Physiologically Based Pharmacokinetic Model-Informed Drug Development for Polatuzumab Vedotin: Label for Drug-Drug Interactions Without Dedicated Clinical Trials. Chen, Y; Ding, H; Girish, S; Jin, J; Li, C; Lu, D; Ma, F; Mao, J; Miles, D; Samineni, D; Shi, R; Wright, M, 2020) | 0.56 |
| " The objective of this study was to develop a framework for leveraging physiologically based pharmacokinetic (PBPK) modeling to predict CYP3A-mediated drug-drug interaction (DDI) potential in the pediatric population using solithromycin as a case study." | ( Leveraging Physiologically Based Pharmacokinetic Modeling and Experimental Data to Guide Dosing Modification of CYP3A-Mediated Drug-Drug Interactions in the Pediatric Population. Carreño, FO; Cohen-Wolkowiez, M; Edginton, AN; Gonzalez, D; Salerno, SN, 2021) | 0.62 |
| " A preliminary physiologically based pharmacokinetic (PBPK) model for drug-drug interactions indicated possible involvement of a metabolite to the perpetrator potential of ketoconazole." | ( Does the circulating ketoconazole metabolite N-deacetyl ketoconazole contribute to the drug-drug interaction potential of the parent compound? Burhenne, J; Foerster, KI; Haefeli, WE; Lehr, T; Mikus, G; Weber, M; Weiss, J, 2022) | 1.23 |
| "The prediction of drug-drug interactions (DDIs) plays critical roles for the estimation of DDI risk caused by inhibition of CYP3A4." | ( Predicting the Drug-Drug Interaction Mediated by CYP3A4 Inhibition: Method Development and Performance Evaluation. Chen, T; Ren, HC; Sai, Y; Tang, L; Yang, CG; Zhang, C, 2021) | 0.62 |
| "In vitro evaluation of the P-glycoprotein (P-gp) inhibitory potential is an important issue when predicting clinically relevant drug-drug interactions (DDIs)." | ( In Vitro Evaluation of P-gp-Mediated Drug-Drug Interactions Using the RPTEC/TERT1 Human Renal Cell Model. Bin, V; Delavenne, X; Hodin, S; Ollier, E; Saib, S, 2022) | 0.72 |
| "Due to health authority warnings and the recommended limited use of ketoconazole as a model inhibitor of cytochrome P450 (CYP) 3A4 in clinical drug-drug interaction (DDI) studies, there is a need to search for alternatives." | ( A Mechanistic Absorption and Disposition Model of Ritonavir to Predict Exposure and Drug-Drug Interaction Potential of CYP3A4/5 and CYP2D6 Substrates. Arora, S; Gardner, I; Jamei, M; Kilford, PJ; Pansari, A; Turner, DB, 2022) | 0.96 |
| "The current model, which incorporates formulation characteristics and mechanistic disposition parameters, can be used to assess the DDI potential of CYP3A4/5 and CYP2D6 substrates administered with a twice-daily dose of 100 mg of ritonavir for 14 days." | ( A Mechanistic Absorption and Disposition Model of Ritonavir to Predict Exposure and Drug-Drug Interaction Potential of CYP3A4/5 and CYP2D6 Substrates. Arora, S; Gardner, I; Jamei, M; Kilford, PJ; Pansari, A; Turner, DB, 2022) | 0.72 |
| " The current intention of the research was to enhance solubility followed by oral bioavailability of IBR using the hot melt extrusion (HME) technique by formulating drug-drug cocrystals (DDCs)." | ( In Silico Screening as a Tool to Prepare Drug-Drug Cocrystals of Ibrutinib-Ketoconazole: a Strategy to Enhance Their Solubility Profiles and Oral Bioavailability. Bangera, PD; Kara, DD; Mehta, CH; Rathnanand, M; Tanvi, K, 2023) | 1.14 |
The bioavailability of a generic preparation of ketoconazole (Zorinax from Xepa-Soul Pattinson, Malaysia) was evaluated in comparison with the innovator product (Nizoral from Janssen Pharmaceutica, Switzerland). The extraction ratio in the liver decreased from 93% to 77% in the control rats.
Male Wistar rats were dosed with miconazole, ketoconazole and itraconazole by gastric intubation once daily for up to 7 days. Theophylline dosage adjustment is probably not necessary for concomitant theophyllines and ketoconzole drug therapy.
| Excerpt | Relevance | Reference |
|---|---|---|
| " The proposed HPLC methods are applied to the analysis of commercial dosage forms (creams) with solid-phase extraction (SPE) procedure, using a diol sorbent, being found to be a convenient technique for the sample preparation giving quantitative drug recovery." | ( HPLC analysis of imidazole antimycotic drugs in pharmaceutical formulations. Andrisano, V; Cavrini, V; Di Pietra, AM; Gatti, R, ) | 0.13 |
| " Cure of the toenails was observed in 79% of the patients treated with the 200 mg dosage and in 26% of those treated with 100 mg at 6 months after therapy." | ( Posttreatment itraconazole levels in the nail. New implications for treatment in onychomycosis. Cauwenbergh, G; De Doncker, P; Heykants, J; Roseeuw, D; Van Cutsem, J; Van de Velde, V; Willems, J; Willemsen, M; Woestenborghs, R, 1992) | 0.28 |
| " The proper duration and dosage and the combination of antifungal drugs have not been clearly defined." | ( [Primary Aspergillus endocarditis. Apropos of a case and review of the international literature]. Cajot, MA; Gosselin, B; Goullard, L; Koussa, A; Marquette, F; Pol, A; Roux, JP; Soots, G; Warembourg, H, 1992) | 0.28 |
| " In this open non-comparative clinical trial, itraconazole was given orally in the dosage of 100 mg per day for 14 consecutive days." | ( Treatment of dermatophytosis with new systemic antifungal agent, itraconazole. Noppakun, N; Phuphaibool, K, 1992) | 0.28 |
| " Liposomal Amphotericin B allowing higher dosage by lower toxicity appears effective as salvage treatment especially in aspergillosis which also responds to Itraconazole available as oral formulation so far." | ( Antifungal treatment strategy in leukemia patients. Büchner, T; Roos, N, 1992) | 0.28 |
| " In vivo, subchronic intraperitoneal dosing with 40 mg/kg ketoconazole or itraconazole to mice had no effect on the antibody response to SRBC as measured by the number of splenic IgM and IgG plaque-forming cells and did not significantly affect the DTH response to oxazolone." | ( Lack of immunosuppression by ketoconazole and itraconazole. Aerts, F; Cools, M; Van Wauwe, J, 1992) | 0.82 |
| " Patients were classified in terms of severity and received itraconazole at the dosage of 200 to 400 mg per day until previously described criteria of cure have been reached." | ( Itraconazole in the treatment of chromoblastomycosis due to Fonsecaea pedrosoi. Bordignon, GF; Cauwenbergh, G; Fillus, JN; Lameira, RP; Purim, KS; Queiroz-Telles, F; Van Cutsem, J, 1992) | 0.28 |
| " The trial also aimed at a possible improvement of the therapy of toxoplasmosis in regard to safety and dosing easiness." | ( [Itraconazole action on Toxoplasma gondii]. Amato Neto, V; Braz, LM; Camargo, ME; Jamra, LM, ) | 0.13 |
| " This requires a significant reduction in cyclosporin dosage regimen which may result in savings of nearly $5,000/year per transplant recipient." | ( Cyclosporin and ketoconazole, drug interaction or therapeutic association? Albengres, E; Tillement, JP, 1992) | 0.63 |
| " One additional cat failed to improve initially, but complete resolution was achieved after the dosage of ketoconazole was doubled." | ( Ketoconazole for treatment of dermatophytosis in cats. Chalmers, SA; Medleau, L, 1992) | 1.94 |
| " Breeding trials after ketoconazole administration resulted in normal fertility and fecundity even at the highest dosage studied." | ( The effect of ketoconazole on endocrine and reproductive parameters in male mice and rats. Cosentino, MJ; Heckman, WR; Kane, BR; Pakyz, RE, ) | 0.8 |
| " However, 600 mg/day may be approaching the upper limits of acceptable dosing for long-term treatment." | ( High-dose itraconazole in the treatment of severe mycoses. Dunn, JF; Fetchick, RJ; Graybill, JR; Hardin, TC; Rinaldi, MG; Sharkey, PK, 1991) | 0.28 |
| " In those treated for two months or longer, the mean total serum IgE level fell from 2,462 U/ml (CI, 752 to 4,202 U/ml) to 502 U/ml (CI, 123 to 880 U/ml) during each course, and the mean daily steroid dosage was decreased to a mean of 24 mg/day (CI, 11 to 37 mg/day)." | ( Adjunctive therapy of allergic bronchopulmonary aspergillosis with itraconazole. Denning, DW; Lewiston, NJ; Stevens, DA; Van Wye, JE, 1991) | 0.28 |
| " However, the wide variation within and between patients suggests that an ITRA-PEL dosage of 400 mg/day may ensure earlier and more consistent therapeutic levels." | ( Comparison of the multiple dose pharmacokinetics of two formulations of itraconazole during remission induction for acute myeloblastic leukaemia. Bradford, CR; Copplestone, JA; Prentice, AG; Warnock, DW, 1991) | 0.28 |
| " In group 2, on 57 of 3316 days (2%), fluconazole in a higher dosage was administered for treatment." | ( Fluconazole prophylaxis of recurrent oral candidiasis in HIV-positive patients. Gentschew, G; Helm, EB; Just-Nübling, G; Meissner, K; Odewald, J; Staszewski, S; Stille, W, 1991) | 0.28 |
| "Ketoconazole action dosed as 400-600 g per day was studied in 12 patients with prostatic metastasizing carcinoma." | ( [Results of a clinical trial of ketoconazole in metastatic prostatic carcinoma]. Morávek, P; Zita, K, 1991) | 2.01 |
| " The concentrations of itraconazole that reversed drug resistance are comparable to the plasma levels achieved by therapeutic dosage used in the treatment of fungal infections." | ( Reversal of daunorubicin resistance in P388/ADR cells by itraconazole. Gollapudi, S; Gupta, S; Kim, J, 1991) | 0.28 |
| " Zidovudine dosage was adjusted 92 times in the other 31 children (52%), mostly due to neutropenia (83%)." | ( Low-dose zidovudine in children with an human immunodeficiency virus type 1 infection acquired in the perinatal period. Blanche, S; Debré, M; Duliege, AM; Griscelli, C; Kouzan, S; Navarette, MS; Rouzioux, C; Seldrup, J; Tardieu, M, 1991) | 0.28 |
| " The same results could not be achieved with the same concentration or dosage of either ketoconazole or fluconazole." | ( Oral and parenteral treatment with itraconazole in various superficial and systemic experimental fungal infections. Comparisons with other antifungals and combination therapy. Van Cutsem, J, 1990) | 0.5 |
| " The feasibility of one-day therapy was assessed in a clinical study in which three different dosage regimens were compared in a total of 552 patients with acute vulvovaginal candidosis: 200 mg twice daily for one day; 200 mg once daily for two days; and 200 mg once daily for three days." | ( Itraconazole: a single-day oral treatment for acute vulvovaginal candidosis. Wesel, S, 1990) | 0.28 |
| " The fixed schedules indicated by pharmacokinetics and clinical studies are one 100 mg capsule daily for 15 days in cases of tinea corporis and tinea cruris and the same dosage for 30 days in cases of tinea pedis and tinea manuum." | ( Itraconazole in common dermatophyte infections of the skin: fixed treatment schedules. Bonifaz, A; Saul, A, 1990) | 0.28 |
| " In order to prevent a mycotic infection in these immunocompromised patients, itraconazole, a new broad-spectrum antimycotic drug of the azole group, was given in an oral dosage of 100 mg day-1 (mean duration of prophylactic treatment 24 months)." | ( Prophylaxis of fungal infections with itraconazole in immunocompromised cancer patients. König, HJ; Mühldorfer, SM, 1990) | 0.28 |
| " Overall, this study demonstrates the value of a dosage of 100 mg of fluconazole or of 400 mg of ketoconazole daily for the management of oropharyngeal candidiasis in patients with cancer." | ( Therapy for oropharyngeal candidiasis in the immunocompromised host: a randomized double-blind study of fluconazole vs. ketoconazole. Aoun, M; Gerard, M; Meunier, F, ) | 0.56 |
| " injected RA from plasma: the half-life of RA increased from 27 min in control-treated animals to 43 min and 76 min after dosing with ketoconazole and R 75 251, respectively." | ( Effects of cytochrome P-450 inhibitors on the in vivo metabolism of all-trans-retinoic acid in rats. Coene, MC; Cools, W; Goossens, J; Monbaliu, J; Van Wauwe, JP, 1990) | 0.48 |
| " Three days of oral dosing with ketoconazole at 200 mg/kg reduced fertility compared to controls." | ( The effect of ketoconazole on fertility of male rats. Martin, A; Vickery, BH; Waller, DP; Zaneveld, LJ, 1990) | 0.92 |
| " Twenty dogs with hyperadrenocorticism (11 with PDH, 9 with adrenocortical tumor) were treated with ketoconazole at a dosage of 15 mg/kg given every 12 hours for a half month to 12 months." | ( Plasma cortisol response to ketoconazole administration in dogs with hyperadrenocorticism. Bruyette, DS; Farver, TB; Feldman, EC; Nelson, RW, 1990) | 0.79 |
| " capitatum are usually sensitive to the azole compounds the explanation may be a too low daily dosage for the treatment of severely immunocompromised hosts." | ( [Trichosporon capitatum septicemia in immunosuppressed patients]. Bergerat, JP; Dufour, P; Herbrecht, R; Koenig, H; Liu, KL; Maloisel, F; Oberling, F; Waller, J, 1990) | 0.28 |
| " She was treated continuously for 6 years with ketoconazole at the same dosage of 200 mg/day." | ( Aneurysm associated with chronic mucocutaneous candidiasis during long-term therapy with ketoconazole. Dompmartin, A; Houtteville, JP; Leroy, D; Theron, J, 1989) | 0.76 |
| " Treatment of invasive aspergillosis required a higher dosage (about 5 mg/kg) and prolonged administration." | ( Experience with itraconazole in cryptococcosis and aspergillosis. Almaviva, M; Cristina, S; De Maria, R; Ferrazzi, P; Fiocchi, R; Langer, M; Negri, C; Scoccia, S; Tortorano, AM; Viviani, MA, 1989) | 0.28 |
| "We have studied the influence of food and dose (50, 100, 200 mg) on the oral systemic availability of the broad spectrum antifungal itraconazole and the pharmacokinetics after repeated dosing of 100 mg in six healthy volunteers." | ( The effects of food and dose on the oral systemic availability of itraconazole in healthy subjects. Gasparini, R; Gauwenbergh, G; Heykants, J; Van Peer, A; Woestenborghs, R, 1989) | 0.28 |
| " Increasing the ketoconazole dosage up to 1,200 mg per day was ineffective in two patients." | ( [Long-term treatment of Cushing's disease using ketoconazole. Possibility of therapeutic escape]. Diop, SN; Duet, M; Firmin, C; Lubetzki, J; Mosse, A; Warnet, A, ) | 0.73 |
| " There is a clear need to obtain quick information on itraconazole plasma levels in order to adapt dosage during prophylactic treatment in immunocompromised patients." | ( Antifungal prophylaxis with itraconazole in prolonged neutropenia: correlation with plasma levels. Boogaerts, MA; De Beule, K; Demuynck, H; Verbist, L; Verhoef, GE; Zachee, P, 1989) | 0.28 |
| " Further studies are needed to determine the optimum dosage and duration of treatment with ketoconazole for this condition." | ( Further studies on the treatment of African histoplasmosis with ketoconazole. Hay, RJ; Mabey, DC, ) | 0.59 |
| " It was concluded that ketoconazole at this dosage is a useful treatment for canine nasal aspergillosis, but is no more effective than thiabendazole." | ( Use of ketoconazole in the treatment of canine nasal aspergillosis. Sharp, NJ; Sullivan, M, 1989) | 1.04 |
| "We have treated 10 patients with histologically diagnosed prostate carcinoma, in states C and D, with orally administered dosage of 1200 mg." | ( [Treatment of advanced prostatic carcinoma with ketoconazole. Our experience in 10 cases]. Carretero González, P; Chuan Nuez, P; Clar Blanch, F; Galan Brotons, A; Gil Salom, M; Santamaría Meseguer, J, ) | 0.39 |
| " bolus dose of cyclosporine either alone or on day seven of a 10-day, 13 mg/kg/day, oral dosing regimen of ketoconazole." | ( Pharmacokinetics of the cyclosporine-ketoconazole interaction in dogs. Burckart, GJ; D'mello, A; Ptachcinski, RJ; Satake, M; Starzl, TE; Takaya, S; Todo, S; Venkataramanan, R, 1989) | 0.76 |
| " Two dosage regimens were tested--200 mg twice a day for 1 day and 200 mg twice a day for 2 days." | ( Itraconazole in the treatment of acute vaginal candidiasis. Barnard, PG; Bloch, B; Burger, GD; Meyer, JS; Parkes, JR; Smythe, E, 1988) | 0.27 |
| " This study could not demonstrate any significant effect of renal dysfunction and hemodialysis or continuous ambulatory peritoneal dialysis treatment upon the pharmacokinetics of itraconazole, and firm conclusions concerning dosing in such patients should await confirmation of our data in a larger patient population." | ( Itraconazole pharmacokinetics in patients with renal dysfunction. Boelaert, J; Daneels, R; De Beule, K; Heykants, J; Matthys, E; Schurgers, M; van Peer, A; Woestenborghs, R, 1988) | 0.27 |
| "Male Wistar rats were dosed with miconazole, ketoconazole and itraconazole by gastric intubation once daily for up to 7 days." | ( Induction potential of antifungals containing an imidazole or triazole moiety. Miconazole and ketoconazole, but not itraconazole are able to induce hepatic drug metabolizing enzymes of male rats at high doses. Heykants, J; Lavrijsen, K; Meuldermans, W; Thijs, D; Van Houdt, J, 1986) | 0.75 |
| " The pharmacologic profiles, mechanisms of action, pharmacokinetics, clinical indications for use, dosage recommendations, side effects, and drug interactions for these agents are presented." | ( The pharmacology of agents used in the treatment of pulmonary mycoses. Borgers, M; Cauwenbergh, G; Vanden Bossche, H, 1986) | 0.27 |
| "The effects of administering ketoconazole at a high dosage (30 mg/kg of body weight/day) and at a low dosage (10 mg/kg/day) on steroidogenesis in the dog were compared." | ( Ketoconazole-induced changes in selected canine hormone concentrations. McDonald, R; Nachreiner, R; Roudebush, P; Willard, MD, 1986) | 2 |
| " It appears that a dosage of 50 mg of itraconazole daily is not adequate for the treatment of these mycoses." | ( Itraconazole in the treatment of superficial mycoses: an open trial of 40 cases. Arias, I; Bonifáz, A; Saúl, A, ) | 0.13 |
| " Since the larger dosage induces a faster response, it should be evaluated further." | ( Itraconazole in the treatment of dermatophytoses: a comparison of two daily dosages. Borghys, A; De Veylder, H; Degreef, H; Duprez, K; Mariën, K; Verhoeve, L, ) | 0.13 |
| " The dosage was 100 mg daily for four to six weeks." | ( Itraconazole in the treatment of tinea corporis: a pilot study. Nuijten, ST; Schuller, JL, ) | 0.13 |
| " The difference between these rates was not significant, but the groups were small and the difference in dosage may ultimately be meaningful in terms of rates of cure." | ( Itraconazole in pityriasis versicolor. Estrada, RA, ) | 0.13 |
| " The sexual partners of one-half of the women were treated with the same dosage of itraconazole; the other men received placebo." | ( Itraconazole in the treatment of vaginal candidosis and the effect of treatment of the sexual partner. Calderón-Márquez, JJ, ) | 0.13 |
| " Almost 50% were women with vaginal candidosis; a dosage of 200 mg per day for three days appeared to be optimal for their treatment." | ( Itraconazole in the treatment of human mycoses: review of three years of clinical experience. Cauwenbergh, G; De Dier, AM; De Doncker, P; Goyvaerts, H; Schuermans, V; Stoops, K, ) | 0.13 |
| " Itraconazole was administered at a daily dosage of 50 mg for six months in the majority of these cases." | ( Oral treatment of paracoccidioidomycosis and histoplasmosis with itraconazole in humans. Galimberti, RL; Koren, F; Negroni, R; Palmieri, O; Tiraboschi, IN, ) | 0.13 |
| " Dosage was 100-200 mg per day, and duration of treatment was based on response." | ( Itraconazole for deep mycoses: preliminary experience in Mexico. De Ovando, F; Lavalle, P; Reynoso, S; Suchil, P, ) | 0.13 |
| " After 7 days repeated dosing liver weight and microsomal protein content were increased in a dose-dependent fashion." | ( The acute and subchronic effects of ketoconazole on hepatic microsomal monooxygenases in the rat. James, OF; Rawlins, MD; Thomson, RG; Williams, FM; Wood, P, 1988) | 0.55 |
| " The in vitro activity of LY121019 is marked by a paradoxical dose-response with isolates of Candida albicans and Candida tropicalis and is influenced by choice of inoculum size, time and temperature of incubation, medium composition, and pH." | ( Influence of in vitro susceptibility testing conditions on the anti-candidal activity of LY121019. Gerarden, T; Pfaller, MA; Wenzel, RP; Yu, M, 1988) | 0.27 |
| " In each case, some dosage adjustment for ketoconazole, or the interacting drug, may be required." | ( Clinical pharmacokinetics of ketoconazole. Daneshmend, TK; Warnock, DW, 1988) | 0.83 |
| " Two reported cases indicate that cyclosporine and ketoconazole can be safely coadministered, provided that the dosage of cyclosporine is reduced appropriately." | ( Use of cyclosporine and ketoconazole without nephrotoxicity in two heart transplant recipients. Clardy, CW; Collins, JA; First, MR; Melvin, DB; Myre, SA; Pesce, AJ; Reising, JM; Schroeder, TJ; Wadhwa, NK; Wolf, RK, ) | 0.69 |
| " In vivo, ketoconazole suppressed the formation of polar RA metabolites by normal rats dosed intrajugularly with 200 ng of [3H]RA." | ( Ketoconazole inhibits the in vitro and in vivo metabolism of all-trans-retinoic acid. Coene, MC; Cools, W; Goossens, J; Lauwers, W; Van Nijen, G; Van Wauwe, JP, 1988) | 2.12 |
| " Once-a-day dosage regimens of ketoconazole in immunocompromised patients may be inappropriate." | ( Ketoconazole pharmacokinetics during chronic dosing in adults with haematological malignancy. Bredow, MT; Daneshmend, TK; Richardson, MD; Slade, RR; Stockley, RJ; Warnock, DW, 1986) | 2 |
| "8%) over a mean treatment period from a minimum of 29 days (pityriasis versicolor) to a maximum of 39 days (tinea pedis) and 150 days (monilial granuloma), with a mean daily dosage of 200 mg in adults and 100 mg in children." | ( Ketoconazole: therapeutic results obtained in the district of Cagliari. Aste, N; Biggio, P; Mulas, P; Orru', A, 1986) | 1.71 |
| " The dose-response curve for cyclosporine was shifted to the left when cyclosporine and ketoconazole were coadministered compared with treatment with cyclosporine alone." | ( Pharmacodynamics of cyclosporine-ketoconazole interaction in mice. Combined therapy potentiates cyclosporine immunosuppression and toxicity. Anderson, JE; Blaschke, TF; Morris, RE, 1987) | 0.78 |
| " Theophylline dosage adjustment is probably not necessary for concomitant theophylline and ketoconazole drug therapy." | ( Effect of chronically administered ketoconazole on the elimination of theophylline in man. Dukes, GE; Galinsky, RE; Heusner, JJ; Rollins, DE; Tolman, KG, 1987) | 0.77 |
| " This suggests that the administration of Ksol may be a useful alternative to dosage increases in situations where low bioavailability of ketoconazole in tablet form is suspected." | ( Pharmacokinetics of ketoconazole administered intravenously to dogs and orally as tablet and solution to humans and dogs. Baxter, JG; Brass, C; Schentag, JJ; Slaughter, RL, 1986) | 0.8 |
| " It was demonstrated from dose-response and time-course experiments that a dose of approximately 10 micrograms/ml ketoconazole was sufficient to inhibit in vitro testicular steroidogenesis." | ( In vitro inhibition of testosterone biosynthesis by ketoconazole. Rajfer, J; Sikka, SC; Swerdloff, RS, 1985) | 0.73 |
| " Amphotericin B and terbinafine possessed intermediate ATP-suppressing activity, and the dose-response and pH-response curves for these compounds suggested their mechanism of ATP suppression differed from that of the active imidazole derivatives." | ( Suppression of ATP in Candida albicans by imidazole and derivative antifungal agents. Abbott, AB; Cheesman, SL; Odds, FC, 1985) | 0.27 |
| " A dosage of 10 to 15 mg/kg of body weight was given once or twice daily with a meal for 11 to 33 weeks." | ( Treatment of cryptococcosis in three cats, using ketoconazole. Martin, RA; Pentlarge, VW, 1986) | 0.53 |
| " After repetitive dosing with ketoconazole, chlordiazepoxide clearance decreased by 38% and was associated with reduced concentrations of its first oxidative metabolite, N-desmethylchlordiazepoxide." | ( Effect of ketoconazole on hepatic oxidative drug metabolism. Brown, MW; Maldonado, AL; Meredith, CG; Speeg, KV, 1985) | 0.96 |
| " Ketoconazole, a systemic antifungal drug, was evaluated in a dosage of 200 mg 8-hourly given orally as an alternative method of lowering serum testosterone levels." | ( High-dose ketoconazole therapy in prostatic cancer. A pilot study. Nicolle, P; Pontin, A; Sarembock, L, 1985) | 1.58 |
| " Because ketoconazole has in-vitro activity against Blastomyces dermatitidis, we administered this agent in a dosage of 400 mg/d to 46 patients with blastomycosis, with 43 patients receiving at least 1 month of therapy." | ( Ketoconazole therapy for endemic blastomycosis. Abernathy, RS; Bradsher, RW; Rice, DC, 1985) | 2.13 |
| "Rats bearing mammary carcinomas induced by N-nitroso-N-methylurea (NMU) were subjected to either no treatment (C), to ovariectomy (O), to continuous ketoconazole dosing at 400 ppm into the diet (K) or to both ovariectomy and ketoconazole dosing (O + K)." | ( Effect of a high dosage of ketoconazole all or not combined with ovariectomy on N-nitroso-N-methylurea-induced mammary cancer in the rat. de Coster, R; Hérin, V; Marsboom, R; van Cauteren, H; van den Berghe, J, 1984) | 0.76 |
| " To achieve therapeutic concentrations of ketoconazole in children we suggest a daily dosage of 7 to 10 mg/kg in two or three divided doses." | ( Pharmacokinetics of ketoconazole and treatment evaluation in candidal infections. Bardare, M; Pietrogrande, MC; Tortorano, AM; Viviani, MA, 1984) | 0.86 |
| " Dosage adjustment is not required in renal failure." | ( Ketoconazole. Mechanism of action, spectrum of activity, pharmacokinetics, drug interactions, adverse reactions and therapeutic use. Van Tyle, JH, ) | 1.57 |
| " The drug was administered orally in a dosage of 200 to 400 mg per day within a period of up to 90 days." | ( Treatment of paracoccidioidomycosis, candidiasis, chromomycosis, lobomycosis, and mycetoma with ketoconazole. Cucé, LC; Sampaio, SA; Wroclawski, EL, 1980) | 0.48 |
| " Initial ketoconazole dosage was 100 mg daily for patients weighing less than 30 kg and 200 mg daily for patients over 30 kg." | ( Successful treatment of chronic mucocutaneous candidiasis with ketoconazole. Ament, ME; Byrne, W; Graybill, J; Rosenblatt, HM; Stiehm, ER, 1980) | 0.92 |
| " Dosage of ketoconazole varied from a single dose of 400 mg to 200--400 mg per day for four weeks." | ( Treatment of pityriasis versicolor with ketoconazole. Borelli, D, ) | 0.79 |
| " The initial dosage was 400 mg per day." | ( Ketoconazole in the treatment of paracoccidioidomycosis and histoplasmosis. Arechavala, A; Galimberti, R; Negroni, R; Robles, AM; Tuculet, MA, ) | 1.57 |
| " Review of these five cases and 31 additional relapsing cases from the literature indicates that fungal endocarditis or endarteritis without surgical treatment, underlying lymphoreticular neoplasm, and amphotericin B dosage of less than 2 g appear to be associated with relapse of PDH." | ( Conditions associated with relapse of amphotericin B-treated disseminated histoplasmosis. Alford, RH; Bradsher, RW; Hawkins, SS; Spickard, WA, 1982) | 0.26 |
| " With no amphotericine B available, treatment first started with high dosage of miconazole which had no effect." | ( [A disseminated form of Histoplasma duboisii histoplasmosis in a Zaïre patient (author's transl)]. Lamey, B, ) | 0.13 |
| " Although this evaluation did not provide clear-cut clinical response data, our results indicate that ketoconazole, in the dosage regimens used, was more effective in patients with histoplasmosis and nonmeningeal cryptococcosis than in patients with blastomycosis and nonmeningeal coccidioidomycosis, and least effective in patients with sporotrichosis." | ( Treatment of systemic mycoses with ketoconazole: emphasis on toxicity and clinical response in 52 patients. National Institute of Allergy and Infectious Diseases collaborative antifungal study. Bowles, C; Cloud, G; Craven, PC; Dismukes, WE; Fields, BT; Gallis, HA; Graybill, JR; Gregg, CR; Kaplowitz, LG; Kerkering, TA; Marier, RL; Medoff, G; Sarosi, GA; Shadomy, S; Stamm, AM; Stevens, DA; Stiller, RL, 1983) | 0.76 |
| " dosage schedule of ketoconazole in vaginal candidosis would give continuously effective levels at the site of infection." | ( Distribution of oral ketoconazole to vaginal tissue. Bisschop, MP; Heykants, JJ; Merkus, JM; Woestenborghs, RJ, 1982) | 0.91 |
| " In some resistant or extremely severe fungal infections antifungal agents can be used in combinations for their synergistic effects, with subsequent reduction of dosage and potential side-effects." | ( [First human case of Drechslera longirostrata mycosis. Spondylodiscitis complicating prosthesis endocarditis. Treatment with combined ketoconazole and amphotericin B]. Brodaty, D; Chapman, A; Drouhet, E; Guilmet, D; Kouvalchouk, JF; Laudet, J; Ziza, JM, 1982) | 0.47 |
| " The concentrations of ketoconazole that inhibited human chorionic gonadotropin stimulation of testicular androgen production and displaced sex steroids from sex hormone-binding globulin were in the range of blood levels found in patients on higher therapeutic dosage regimens." | ( Ketoconazole inhibition of testicular secretion of testosterone and displacement of steroid hormones from serum transport proteins. Boyden, TW; Galgiani, JN; Grosso, DS; Johnson, DG; Pamenter, RW; Stevens, DA, 1983) | 2.02 |
| " The drug was administered orally in the dosage of 200 mg/m2 of body surface per day for two weeks to cancer patients with oral candidiasis." | ( Ketoconazole and candidiasis: a controlled study. Bartley, DL; Hughes, WT; Patterson, GG; Tufenkeji, H, 1983) | 1.71 |
| "The pharmacology, microbiology, pharmacokinetics, clinical use, adverse effects, dosage and administration, and drug interactions of ketoconazole are reviewed." | ( Evaluation of ketoconazole. Sohn, CA, ) | 0.7 |
| " The lack of major effects on testosterone levels long term at this dosage probably explain why few androgen-related side effects with this drug were previously reported." | ( Site of action of low dose ketoconazole on androgen biosynthesis in men. Brugmans, J; DeCoster, R; Santen, RJ; Symoens, J; Van den Bossche, H, 1983) | 0.56 |
| " A daily dosage from 7 to 10 mg/Kg, in two or three administrations, is suggested to obtain therapeutic levels in children." | ( [Ketoconazole treatment of candidiasis in children: clinico-pharmacokinetic study]. Bardare, M; Cohen, E; Pietrogrande, MC; Tortorano, AM; Viviani, MA, ) | 1.04 |
| " Ketoconazole given in a dosage of 400 mg daily or more may inhibit testosterone biosynthesis." | ( [Side effects of ketoconazole]. Haneke, E, 1983) | 1.52 |
| " In view of persistent anomalies of cellular immunity and complete deficiency in serum and salivary IgA, treatment with ketoconazole at the same dosage level has now been continuously pursued for 30 months without any evidence of toxicity." | ( [Monilial granuloma treated successfully with ketoconazole over a period of 30 months]. Deschamps, P; Leroy, D; Mahoudeau, J; Michel, M; Vion, M, 1984) | 0.73 |
| " Analysis of data from previous studies in our laboratories shows that in the absence of intestinal metabolism, cyclosporine absorption from its presently available dosage form averages at least 65% +/- 12% in healthy volunteers and 77% +/- 19% in kidney transplant patients." | ( Differentiation of absorption and first-pass gut and hepatic metabolism in humans: studies with cyclosporine. Benet, LZ; Gomez, DY; Gupta, SK; Hebert, MF; Rowland, M; Wacher, VJ; Wu, CY, 1995) | 0.29 |
| "5 and 24 h following single and multiple dosing regimens with either KC or DAKC indicated that KC was readily metabolized to DAKC whereas, DAKC appeared to be recalcitrant to metabolism and accumulated in the liver." | ( Ketoconazole-induced hepatic phospholipidosis in the mouse and its association with de-N-acetyl ketoconazole. Menzies, A; Mueller, R; Pontefract, R; Whitehouse, LW, ) | 1.57 |
| " Two potential ways of overcoming decreased plasma levels are suggested by the explanations for rapid elimination of ATRA: administration of a P-450 inhibitor such as ketoconazole to block oxidation of the drug, or use of an intermittent dosing schedule." | ( Pharmacokinetics of all-trans-retinoic acid: clinical implications in acute promyelocytic leukemia. Adamson, PC, 1994) | 0.48 |
| "Male Sprague-Dawley rats had their bile ducts cannulated and were dosed with [3H]taxol (2 mg/kg, 68-77 microCi/mg) as a continuous intravenous infusion for 6 hr so that the plasma concentrations, tissue distribution, metabolism, and biliary secretion of taxol could be studied." | ( Effect of cimetidine, probenecid, and ketoconazole on the distribution, biliary secretion, and metabolism of [3H]taxol in the Sprague-Dawley rat. Collins, JM; Egorin, MJ; Erkmen, K; Jamis-Dow, CA; Klecker, RW; Parker, RJ; Stevens, R, ) | 0.4 |
| " The topical agents are available in assorted dosage forms with varying degrees of efficacy and patient acceptability." | ( Treatment of oropharyngeal candidiasis in HIV-positive patients. Greenspan, D, 1994) | 0.29 |
| " These findings may have implications for dosing antifungal agents in systemic yeast infections." | ( The postantibiotic effect of antifungal agents against common pathogenic yeasts. Craig, WA; Gudmundsson, S; Turnidge, JD; Vogelman, B, 1994) | 0.29 |
| " Twenty-four subjects received oral fluconazole in a dosage of 3 mg/kg/day and 22 subjects received oral ketoconazole in a dosage of 7 mg/kg/day." | ( Fluconazole versus ketoconazole in the treatment of oropharyngeal candidiasis in HIV-infected children. Multicentre Study Group. Hernández-Sampelayo, T, 1994) | 0.83 |
| " Twelve healthy male volunteers received each of 4 dosing regimens: 200 mg itraconazole alone, 200 mg itraconazole and famotidine, 100 mg fluconazole alone, and 100 mg fluconazole and famotidine." | ( Short report: the absorption of fluconazole and itraconazole under conditions of low intragastric acidity. Hudson, M; Lim, SG; Pounder, RE; Sawyerr, AM; Sercombe, J, 1993) | 0.29 |
| " However, continuous oral dosing results in progressive decline in plasma drug concentrations, which is associated with relapse and resistance to this retinoid." | ( Constitutive variability in the pharmacokinetics of the natural retinoid, all-trans-retinoic acid, and its modulation by ketoconazole. DeGrazia, F; Francis, PA; Huselton, C; Kris, MG; Muindi, JR; Orazem, JP; Rigas, JR; Warrell, RP; Young, CW, 1993) | 0.49 |
| "Ten patients with eumycetoma were treated with oral ketoconazole in the dosage of 400mg/day for 8 to 24 months." | ( Treatment of eumycetoma with ketoconazole. Venugopal, PV; Venugopal, TV, 1993) | 0.83 |
| " Adrenolytic treatment with ketoconazole (400 mg daily) caused symptoms of adrenal insufficiency, but a reduced dosage of 200 mg daily lowered the cortisol level to between 5 and 11 micrograms/dl and normalized the blood pressure and clinical signs of Cushing's syndrome disappeared." | ( [Bilateral massive macronodular adrenal gland hyperplasia. A rare cause of Cushing's syndrome]. Allolio, B; Diehl, KL; Reincke, M; Strohm, M; Theiss, M, 1994) | 0.58 |
| " Case reports and studies demonstrate decreased dosage requirements of cyclosporine sodium, methylprednisolone sodium succinate, and possibly anticoagulants and phenytoin after ketoconazole or fluconazole administration, suggesting hepatic enzyme inhibition." | ( Ketoconazole and fluconazole drug interactions. Baciewicz, AM; Baciewicz, FA, 1993) | 1.92 |
| " In both studies addition of ketoconazole to cyclosporine-treated patients resulted in significant inhibition of cyclosporine metabolism and decrease in dosage in patients followed for up to four years." | ( Cyclosporine-ketoconazole interaction. Long-term follow-up and preliminary results of a randomized trial. Alexander, JW; First, MR; Hariharan, S; Michael, A; Schroeder, TJ; Weiskittel, P, 1993) | 0.95 |
| " Our results suggest that fresh serum positively influenced PAFE which may be an important factor in determining the dosing regimen for infection by yeasts." | ( Influence of human serum on the postantifungal effect of four antifungal agents on Candida albicans. García, MT; Lima, JE; Mínguez, F; Prieto, J, ) | 0.13 |
| "The stability of drugs commonly prescribed for use in oral liquid dosage forms but not commercially available as such was studied." | ( Stability of ketoconazole, metolazone, metronidazole, procainamide hydrochloride, and spironolactone in extemporaneously compounded oral liquids. Allen, LV; Erickson, MA, 1996) | 0.66 |
| " A sensitivity analysis assessing alternative dosing regimens and a rank order stability analysis investigating the effects of length of treatment, success rates, relapse rates, and drug acquisition costs on overall results were also conducted." | ( Pharmacoeconomic analysis of oral therapies for onychomycosis: a US model. Marchetti, A; McGhan, WF; Neugut, AI; Piech, CT; Smith, BT, ) | 0.13 |
| " This dosage was reduced to 200 mg/day for patients below 12 years of age." | ( A randomized clinical trial of topical paromomycin versus oral ketoconazole for treating cutaneous leishmaniasis in Turkey. Baydar, I; Ozgoztasi, O, 1997) | 0.54 |
| " orally in divided dosage for 30 days." | ( Combination therapy in Kala-azar. Jha, S; Jha, TK; Singh, IJ; Singh, NK, 1995) | 0.29 |
| " We report a case of fulminant adrenal crisis precipitated by ketoconazole given on a 6-hour dosing schedule in a patient with nerve root compression secondary to prostatic metastases." | ( Ketoconazole-induced adrenal crisis in a patient with metastatic prostatic adenocarcinoma: case report and review of the literature. Ahmann, FR; Dalkin, BL; Sarver, RG, 1997) | 1.98 |
| " Many transplant centres routinely use drugs ("cyclosporin-sparing agents') to allow a reduction in the dosage of cyclosporin while maintaining therapeutic blood cyclosporin concentrations." | ( The use of other drugs to allow a lower dosage of cyclosporin to be used. Therapeutic and pharmacoeconomic considerations. Jones, TE, 1997) | 0.3 |
| " Dogs were dosed daily with ketoconazole at dose of 100 mg ketoconazole per dog (approximately 10 mg/kg) for 5 days prior to the initiation of coadministration of SC-52151 for 15 days." | ( Improvement of bioavailability of the HIV protease inhibitor SC-52151 in the beagle dog by coadministration of the CYP3A4 inhibitor, ketoconazole. Salamon, CM; Schoenhard, GL; Snook, SS; Stolzenbach, JC; Yuan, JH, 1997) | 0.79 |
| " Close monitoring of cyclosporine levels is imperative when adding ketoconazole to cyclosporine, and once the dosage adjustments are complete, the addition of a third drug that interacts with either cyclosporine or ketoconazole could result in an unexpected rejection episode or toxic cyclosporine side effect." | ( Considerations for using ketoconazole in solid organ transplant recipients receiving cyclosporine immunosuppression. Chapman, SA; Kamps, MA; Lake, KD; Marshall, PS; Milfred, SK; Solbrack, DF, 1996) | 0.83 |
| "To report the successful reduction of cyclosporine dosage with adjunctive ketoconazole in a patient with birdshot retinochoriodopathy." | ( Reduction of cyclosporine dosage with ketoconazole in a patient with birdshot retinochoroidopathy. Silverstein, BE; Wong, IG, 1998) | 0.8 |
| " Her cyclosporine dosage was reduced to 40 mg per day from 200 mg per day, an 80% reduction." | ( Reduction of cyclosporine dosage with ketoconazole in a patient with birdshot retinochoroidopathy. Silverstein, BE; Wong, IG, 1998) | 0.57 |
| "Cyclosporine dosage may be reduced considerably in patients with uveitis who use adjunctive ketoconazole." | ( Reduction of cyclosporine dosage with ketoconazole in a patient with birdshot retinochoroidopathy. Silverstein, BE; Wong, IG, 1998) | 0.79 |
| " In addition, the short treatment times (< 3 months) and intermittent dosing schedules are likely to enhance compliance and reduce the costs of therapy." | ( Onychomycosis: pathogenesis, diagnosis, and management. Elewski, BE, 1998) | 0.3 |
| " For patients administered concomitant cyclosporine, ketoconazole, and diltiazem, the dosage of cyclosporine, if it is administered alone, should be 20% to achieve the same blood concentrations." | ( Effect of metabolic inhibitors on cyclosporine pharmacokinetics using a population approach. McLachlan, AJ; Tett, SE, 1998) | 0.55 |
| " Zolpidem-induced benzodiazepine agonist effects (increased electrocardiographic beta activity, digit-symbol substitution test impairment, and delayed recall) during the first 4 hours after dosage were enhanced by ketoconazole but not by itraconazole or fluconazole." | ( Kinetic and dynamic interaction study of zolpidem with ketoconazole, itraconazole, and fluconazole. Counihan, M; Durol, AL; Graf, JA; Greenblatt, DJ; Harmatz, JS; Mertzanis, P; Roth-Schechter, B; Shader, RI; von Moltke, LL, 1998) | 0.73 |
| " Further, these results may have an important bearing on dosage regimens currently employed in treating oral candidosis." | ( Adhesion of oral Candida albicans isolates to denture acrylic following limited exposure to antifungal agents. Ellepola, AN; Samaranayake, LP, 1998) | 0.3 |
| "To evaluate methodology for in vivo interaction studies of benzodiazepines (BZs) and ketoconazole (KCZ) in animal models, this study assessed the pharmacokinetics and electroencephalographic (EEG) effect of KCZ, and suitable dosage regimens of KCZ to maintain sufficiently high KCZ concentrations to inhibit metabolism of BZs in rats." | ( Pharmacokinetics and electroencephalographic effects of ketoconazole in the rat. Durol, AL; Greenblatt, DJ; Kotegawa, T; Laurijssens, BE, 1999) | 0.77 |
| " Male offsprings display a higher incidence of epididymal and testicular lesions than generally seen with flutamide, P, or V even at high dosage levels." | ( Administration of potentially antiandrogenic pesticides (procymidone, linuron, iprodione, chlozolinate, p,p'-DDE, and ketoconazole) and toxic substances (dibutyl- and diethylhexyl phthalate, PCB 169, and ethane dimethane sulphonate) during sexual differen Cooper, RL; Gray, LE; Lambright, C; Mann, P; Ostby, J; Price, M; Wolf, C, ) | 0.34 |
| " The dosage and therapeutic duration were as follows: Flu 200-400 mg daily for 1-8 weeks in 34 patients with fungal infection and 150 mg as a single dose in 30 patients with fungal vaginitis; Keto 400 mg daily for 1-8 weeks in 30 patients with fungal diseases and for 5 days in 30 patients with fungal vaginitis." | ( [Fluconazole versus ketoconazole in systemic fungal infection: a double-blind randomized study]. Liang, D; Lu, Y; Zhang, H, 1997) | 0.62 |
| "A fixed hMG dosage was initiated on cycle days 5-9 in both of the study cycles." | ( Attenuation of ovarian response by low-dose ketoconazole during superovulation in patients with polycystic ovary syndrome. Barr, I; Diamant, YZ; Eldar-Geva, T; Gal, M; Margalioth, EJ; Orly, J, 1999) | 0.56 |
| " All three benzodiazepines were susceptible to drug interactions, but oral dosing of midazolam and triazolam resulted in greater alterations in the pharmacokinetic parameters than alprazolam due to their larger presystemic extraction." | ( Pharmacokinetic and pharmacodynamic consequences of metabolism-based drug interactions with alprazolam, midazolam, and triazolam. Balian, JD; Flockhart, DA; Yuan, R, 1999) | 0.3 |
| " In two similar experiments, weanling female rats were dosed for 20 days by gavage with vehicle (0." | ( Evaluation of the EDSTAC female pubertal assay in CD rats using 17beta-estradiol, steroid biosynthesis inhibitors, and a thyroid inhibitor. Carney, EW; Crissman, JW; Marty, MS, 1999) | 0.3 |
| " Dosing extended over postnatal days (pnd) 22-35, 36-50, 36-55 and 22-35, with recovery to pnd 55 or 22-55." | ( The peripubertal male rat assay as an alternative to the Hershberger castrated male rat assay for the detection of anti-androgens, oestrogens and metabolic modulators. Ashby, J; Lefevre, PA, ) | 0.13 |
| "Budesonide is a glucocorticosteroid used in the treatment of, for example, inflammatory bowel diseases, with a recommended once-daily morning dosing regimen." | ( Reduction of the inhibitory effect of ketoconazole on budesonide pharmacokinetics by separation of their time of administration. Seidegård, J, 2000) | 0.58 |
| " For example, human terfenadine hepatic extraction goes from 95% in the absence of a competitive inhibitor to 35% in the presence of one (ketoconazole, 200 mg po Q 12 h dosed to steady-state)." | ( Cytochrome P450 3A4 in vivo ketoconazole competitive inhibition: determination of Ki and dangers associated with high clearance drugs in general. Boxenbaum, H, ) | 0.63 |
| " We compared cumulative CCK dose-response relationship in control cells and in cells where P450 had been induced by prior injection of animals with beta-naphthoflavone." | ( Pharmacological evaluation of the role of cytochrome P450 in intracellular calcium signalling in rat pancreatic acinar cells. Bruce, JI; Elliott, AC, 2000) | 0.31 |
| " Blood samples were collected over the daytime 12-hour dosing interval of the protease inhibitors at baseline (period 1, day 0) and after 10 days of coadministration of 200 mg (n = 6) or 400 mg (n = 6) of ketoconazole once daily (period 2, day 10)." | ( Effect of ketoconazole on ritonavir and saquinavir concentrations in plasma and cerebrospinal fluid from patients infected with human immunodeficiency virus. Cameron, DW; Gallicano, K; Khaliq, Y; Kravcik, S; Venance, S, 2000) | 0.9 |
| " Furthermore, no adjustment of citalopram dosage should be necessary in most patients who receive the drug in combination with a CYP3A4 inhibitor." | ( Lack of effect of a single dose of ketoconazole on the pharmacokinetics of citalopram. Abramowitz, W; Gutierrez, M, 2001) | 0.59 |
| " A newly recognized phenomenon known as the post-antifungal effect implies that antifungals, even at sub-therapeutic concentrations, may suppress the virulent attributes of yeasts, especially intra-orally where topical drug levels fluctuate dramatically during dosing intervals." | ( Antimycotic agents in oral candidosis: an overview: 2. Treatment of oral candidosis. Ellepola, AN; Samaranayake, LP, 2000) | 0.31 |
| "9 yr) underwent GnRH dose-response studies at baseline and after treatment with dexamethasone (0." | ( Differential regulation of gonadotropin secretion by testosterone in the human male: absence of a negative feedback effect of testosterone on follicle-stimulating hormone secretion. Boepple, PA; Crowley, WF; DeCruz, S; Hayes, FJ; Seminara, SB, 2001) | 0.31 |
| " Recently, this assay was evaluated by several laboratories using a variety of dosing schemes." | ( Evaluation of the male pubertal onset assay to detect testosterone and steroid biosynthesis inhibitors in CD rats. Carney, EW; Crissman, JW; Marty, MS, 2001) | 0.31 |
| " For patientson ketoconazole, the absorption profile is already optimized and no dosage alteration seems necessary." | ( Pharmacokinetics of cyclosporine in heart transplant recipients receiving metabolic inhibitors. Akhlaghi, F; Kaan, A; Keogh, AM; McLachlan, AJ, 2001) | 0.66 |
| " Steady state oral pharmacokinetic profiles were obtained between 1 and 3 months after transplant while patients were receiving twice daily dosing of tacrolimus to maintain whole blood levels between 10 and 20 ng/ml." | ( The effect of gut metabolism on tacrolimus bioavailability in renal transplant recipients. Alloway, RR; Gaber, AO; Johnson, JA; Tuteja, S, 2001) | 0.31 |
| "Pityriasis versicolor can be treated by a single or multiple dosage regime of ketoconazole as well as by fluconazole." | ( Comparative efficacy of ketoconazole and fluconazole in the treatment of pityriasis versicolor: a one year follow-up study. Baruah, MC; Bhogal, CS; Singal, A, 2001) | 0.85 |
| " Thus, in agreement with the negative results from acute dosing studies in primates and humans, chronic ketoconazole treatment does not appear to reduce cocaine or opioid use in humans maintained on methadone." | ( Ketoconazole increases cocaine and opioid use in methadone maintained patients. Feingold, A; Gonsai, K; Kosten, TR; Oliveto, A; Sevarino, KA, 2002) | 1.97 |
| " Micromeritic investigations were carried out on microcapsules in order to standardize the microcapsule product and to optimize the pilot production of the dosage forms prepared with these microcapsules." | ( Sustained release bioadhesive effervescent ketoconazole microcapsules tabletted for vaginal delivery. Ertan, G; Güneri, T; Karasulu, HY; Sanal, E; Taneri, F, ) | 0.39 |
| " Serial plasma, urine, and feces samples were obtained up to 500 hours after dosing and analyzed for irinotecan, metabolites (7-ethyl-10-hydroxycamptothecin [SN-38], SN-38 glucuronide [SN-38G], and APC), and ketoconazole by high-performance liquid chromatography." | ( Modulation of irinotecan metabolism by ketoconazole. de Bruijn, P; Kehrer, DF; Mathijssen, RH; Sparreboom, A; Verweij, J, 2002) | 0.77 |
| " The exercise aids in integrating all the knowledge across the drug development to suggest rationale dosing strategies; effectively communicating the impact of the prognostic factors to the clinicians/regulators; and protect against any intellectual losses due to development team changes." | ( Application of modeling and simulation to integrate clinical pharmacology knowledge across a new drug application. Gobburu, JV; Sekar, VJ, 2002) | 0.31 |
| " For the current studies, male rats were dosed for 15 days via oral gavage and euthanized on the morning of test day 15." | ( Evaluation of a 15-day screening assay using intact male rats for identifying steroid biosynthesis inhibitors and thyroid modulators. Frame, SR; Ladics, GS; O'Connor, JC, 2002) | 0.31 |
| " Column chromatography methodology was developed to separate lopinavir from ritonavir starting from the commercially available lopinavir-ritonavir combination dosage form." | ( Apparent mechanism-based inhibition of human CYP3A in-vitro by lopinavir. Greenblatt, DJ; Harmatz, JS; Hesse, LM; Richert, C; von Moltke, LL; Weemhoff, JL, 2003) | 0.32 |
| " Profiles of blood glucose concentration following repaglinide dosing were altered by less than 8% by both ketoconazole and rifampicin." | ( Influence of drugs interacting with CYP3A4 on the pharmacokinetics, pharmacodynamics, and safety of the prandial glucose regulator repaglinide. Hansen, KT; Hatorp, V; Thomsen, MS, 2003) | 0.53 |
| " The method is applicable to the assay of the three drugs under investigation in different dosage forms and the results are in good agreement with those obtained by the official methods (USP and JP)." | ( Quantitative determination of some pharmaceutical piperazine derivatives through complexation with iron(III) chloride. Abdel-Gawad, FM; Abdel-Hamid, SM; Abou-Attia, FM; Issa, YM, 2003) | 0.32 |
| " This article reviews recent pertinent data with regard to dosing guidelines, efficacy, and toxicities of available systemic antifungal agents in the newborn." | ( Antifungal pharmacotherapy for neonatal candidiasis. Bliss, JM; Gigliotti, F; Wellington, M, 2003) | 0.32 |
| " To generate a ketoconazole dosing regimen, the pharmacokinetics of ketoconazole were first determined in the monkey and were found to be consistent with that previously described in the rat, dog, and human." | ( Development of an in vivo preclinical screen model to estimate absorption and first-pass hepatic extraction of xenobiotics. II. Use of ketoconazole to identify P-glycoprotein/CYP3A-limited bioavailability in the monkey. Azzarano, LM; Kehler, JR; McSurdy-Freed, JE; Morgan, JA; Proksch, JW; Smith, BR; Stelman, GJ; Ward, KW; Zeigler, KS, 2004) | 0.88 |
| " While griseofulvin was effective to cause > 50% growth inhibition only at higher dosage of 400 ppm." | ( Invitro drug sensitivity of Trichophyton species against griseofulvin and ketoconazole. Bajpai, R; Dodia, S; Singh, BG, ) | 0.36 |
| " The proposed methods were used for determination of ketoconazole in commercial pharmaceutical dosage forms (tablets and creams)." | ( Comparison of capillary zone electrophoresis and high performance liquid chromatography methods for quantitative determination of ketoconazole in drug formulations. Agbaba, D; Cudina, O; Janković, I; Velikinac, I; Vladimirov, S, 2004) | 0.78 |
| " A biphasic dose-response relationship was observed between ketoconazole exposure and hepatic CYP1A-mediated ethoxyresorufin O-deethylase (EROD) activity in rainbow trout in vitro and in vivo, implying that higher doses of ketoconazole inhibit CYP1A activities." | ( Effects of the antifungal imidazole ketoconazole on CYP1A and CYP3A in rainbow trout and killifish. Celander, MC; Hegelund, T; Ottosson, K; Rådinger, M; Tomberg, P, 2004) | 0.84 |
| " This experiment was therefore designed to determine the effects of acute, repeated and chronic ketoconazole administration on corticotropin-releasing hormone (CRH) content in hypothalamic and extra-hypothalamic brain sites in rats following the same dosing regimen that we use in our behavioral studies." | ( Effects of acute and chronic ketoconazole administration on hypothalamo--pituitary--adrenal axis activity and brain corticotropin-releasing hormone. Goeders, NE; Smagin, GN, 2004) | 0.83 |
| " infused or orally dosed ATRA--increased the mean concentration-time curve value by 160% and 78%, respectively." | ( Effect of cytochrome P450 inhibitors (diethyl dithiocarbamate, ketoconazole and grapefruit juice) on the pharmacokinetics of all-trans-retinoic acid. Araico, A; Cárcel-Trullols, J; Peris, JE; Saadeddin, A; Torres-Molina, F, 2004) | 0.56 |
| " Dose-response curves for fluoxetine (0." | ( Synergistic interaction between ketoconazole and several antidepressant drugs with allopregnanolone treatments in ovariectomized Wistar rats forced to swim. García, JP; Jaramillo, MT; Lopez, JI; Molina-Hernández, M; Tellez-Alcántara, NP, 2004) | 0.61 |
| " The dosage of 150 mg once weekly for 6 months was recommended, considering both effectiveness and economy." | ( Combination therapy of once-weekly fluconazole (100, 150, or 300 mg) with topical application of ketoconazole cream in the treatment of onychomycosis. Chen, X; Hiruma, M; Ogawa, H; Shiraki, Y, 2004) | 0.54 |
| " The model improves the accuracy of predicting the inhibitory effect of increasing KTZ dosing on MDZ PK by incorporating a saturable KTZ efflux from the site of enzyme inhibition in the liver." | ( Stochastic prediction of CYP3A-mediated inhibition of midazolam clearance by ketoconazole. Chien, JY; Ernest, CS; Gorski, JC; Hall, SD; Lucksiri, A; Wrighton, SA, 2006) | 0.56 |
| " This makes precise dosing difficult to achieve clinically, which may compromise safe therapy." | ( Ketoconazole renders poor CYP3A phenotype status with midazolam as probe drug. Fan, L; Goh, BC; Lee, HS; Lee, SC; Ong, AB; Soo, R; Sukri, N; Tham, LS; Wang, L; Yong, WP, 2006) | 1.78 |
| " No dosage adjustment should be required when lasofoxifene is coadministered with ketoconazole, fluconazole, paroxetine or other agents that inhibit these CYP enzymes." | ( Effects of three cytochrome P450 inhibitors, ketoconazole, fluconazole, and paroxetine, on the pharmacokinetics of lasofoxifene. Bramson, C; Gardner, M; Milton, A; Ouellet, D; Randinitis, E; Remmers, AE; Roman, D, 2007) | 0.83 |
| "CompritolR888 ATO (glycerol behenate) is widely used as a pharmaceutical excipient in the field of solid dosage forms due to its lubricating properties." | ( Polymorphic behaviour of Compritol888 ATO as bulk lipid and as SLN and NLC. Mehnert, W; Müller, RH; Souto, EB, 2006) | 0.33 |
| " The strains susceptibility to K (RO4 1400 Janssen) was estimated with the own system based on the dose-response curves; the minimal inhibitory concentration (MIC) values were canculated." | ( [The sensitivity to ketoconazole of Candida strains isolated from the digestive tract ontocenoses in children]. Horwatt-Bozyczko, E; Kurnatowska, A; Kurnatowski, M; Wasowska-Królikowska, K, 2001) | 0.63 |
| " The enzyme induction potential of pradefovir was evaluated in rats following multiple oral dosing and in primary cultures of human hepatocytes." | ( Metabolic activation of pradefovir by CYP3A4 and its potential as an inhibitor or inducer. Benetton, S; Fang, C; Lin, CC; Xu, GF; Yeh, LT, 2006) | 0.33 |
| "Variable interindividual expression of cytochrome P450 3A presents a challenge in dosing drugs." | ( Drug-metabolizing enzyme inhibition by ketoconazole does not reduce interindividual variability of CYP3A activity as measured by oral midazolam. Bertino, JS; Chen, M; Nafziger, AN, 2006) | 0.6 |
| " Specifically, a microbial natural product library was screened for hits that synergize the effect of a low dosage of ketoconazole (KTC) that alone shows little detectable fungicidal activity." | ( High-throughput synergy screening identifies microbial metabolites as combination agents for the treatment of fungal infections. An, R; Bian, J; Chen, X; Chen, Z; Dai, H; Fu, C; Gao, H; Goodfellow, M; Huang, R; Jiang, Y; Kuai, J; Liu, J; Liu, Z; Min, F; Pei, G; Song, Y; Sun, H; Sun, N; Wang, J; Yan, K; Yang, K; You, J; Yu, Z; Zhang, L; Zhang, S; Zhang, X; Zhang, Y; Zhao, W; Zheng, C; Zhou, G; Zhuo, Y, 2007) | 0.55 |
| " Depending on the intended indication and dosing regimen, PPL can delay or stop development of a compound in the drug discovery process." | ( Evaluation of a published in silico model and construction of a novel Bayesian model for predicting phospholipidosis inducing potential. Gehlhaar, D; Greene, N; Johnson, TO; Pelletier, DJ; Tilloy-Ellul, A, ) | 0.13 |
| " Because loss of PXR maintains blood levels of paclitaxel upon chronic dosing, ketoconazole analogues may also serve to preserve paclitaxel blood levels on chronic dosing of drugs." | ( Activated pregnenolone X-receptor is a target for ketoconazole and its analogs. Baker, SD; Huang, H; Kalpana, G; Li, H; Mani, S; Redinbo, MR; Sinz, M; Staudinger, J; Teotico, DG; Wang, H, 2007) | 0.82 |
| "Multiple oral dosing of ketoconazole dramatically altered the pharmacokinetics of ivermectin in dogs leading to an increase in systemic exposure to the drug." | ( Multiple oral dosing of ketoconazole increases dog exposure to ivermectin. Alvinerie, M; Hugnet, C; Lespine, A, 2007) | 0.95 |
| "Fixed dosing was found to be feasible, without increased variability of clearance or neutrophil toxicity compared to BSA-based dosing." | ( A phase I study of docetaxel with ketoconazole modulation in patients with advanced cancers. Goh, BC; Lee, HS; Lee, SC; Soo, R; Sukri, N; Tham, LS; Wang, LZ; Wong, CI; Yong, WP, 2008) | 0.63 |
| "A cremophor mixed micelle formulation of saquinavir alone, or co-administered with P-gp/CYP modulators, verapamil, ketoconazole or cyclosporine, was dosed intraduodenally in the mesenteric lymph duct cannulated anaesthetized rat model." | ( An examination of the effect of intestinal first pass extraction on intestinal lymphatic transport of saquinavir in the rat. Griffin, BT; O'Driscoll, CM, 2008) | 0.56 |
| " Lipid granules of KTZ prepared with Compritol 888 ATO could be proposed as a new KTZ solid dosage form with optimum dissolution and therapeutic characteristics." | ( In vitro release--in vivo microbiological and toxicological studies on ketoconazole lipid granules. Ay, Z; Durmaz, G; Ertan, G; Gokce, EH; Gokce, G; Guneri, T; Hilmioglu, S; Metin, DY; Ozer, O; Ozyazici, M; Ozyurt, D; Pekcetin, C; Yalcin, A, 2007) | 0.57 |
| "For the parent compound, ciclesonide, no changes in the pharmacokinetic parameter estimates--the area under the serum concentration-time curve during the dosage interval (AUC(tau)), maximum serum concentration (C(max)) and time to reach the C(max)--were observed." | ( Effect of coadministered ketoconazole, a strong cytochrome P450 3A4 enzyme inhibitor, on the pharmacokinetics of ciclesonide and its active metabolite desisobutyryl-ciclesonide. Böhmer, GM; Drollmann, A; Gleiter, CH; Nave, R, 2008) | 0.65 |
| " The Jonckheere-Terpstra test was used to test for an ordinal dose-response trend between the DIO-902 doses and placebo." | ( Safety profile and metabolic effects of 14 days of treatment with DIO-902: results of a phase IIa multicenter, randomized, double-blind, placebo-controlled, parallel-group trial in patients with type 2 diabetes mellitus. Ahmann, AJ; Arauz-Pacheco, CJ; Rendell, M; Schwartz, SL; Thomas, A; Welles, BR, 2008) | 0.35 |
| " In vivo assessment of CYP1A2 and CYP3A4 activities, perhaps by phenotyping approaches, could assist the optimization of CLZ dosage and minimize pharmacokinetic interactions with coadministered drugs." | ( Interindividual variation in relative CYP1A2/3A4 phenotype influences susceptibility of clozapine oxidation to cytochrome P450-specific inhibition in human hepatic microsomes. D'Esposito, F; Edwards, RJ; Murray, M; Ramzan, I; Zhang, WV, 2008) | 0.35 |
| " dosing with SV alone." | ( Effect of oral ketoconazole on oral and intravenous pharmacokinetics of simvastatin and its acid in cynomolgus monkeys. Fukuzaki, K; Kume, T; Nii, K; Ogasawara, A; Ueda, A; Utoh, M; Yoshikawa, T, 2009) | 0.71 |
| " Ketoconazole strongly inhibited CYP3A4-mediated terfenadine metabolism in vitro, and the method predicted 6- to 37-fold increase of terfenadine AUC by the concomitant dosing of ketoconazole, which reasonably well agreed with the observed 13- to 59-fold increase of AUC in clinical studies." | ( A novel approach to the prediction of drug-drug interactions in humans based on the serum incubation method. Chiba, M; Ishii, Y; Shibata, Y; Takahashi, H, 2008) | 1.26 |
| " The objectives of this study were to investigate the effect of ketoconazole on the pharmacokinetics of saquinavir/ritonavir and vice versa using the approved dosage regimens of saquinavir/ritonavir at 1,000/100 mg twice daily and ketoconazole at 200 mg once daily." | ( Drug-drug interaction study of ketoconazole and ritonavir-boosted saquinavir. Bour, F; Kaeser, B; Schmitt, C; Zandt, H; Zhang, X; Zwanziger, E, 2009) | 0.88 |
| " The influence of solubilizers on the aqueous solubility of the itraconazole, ketoconazole and miconazole was investigated in order to enhance their solubility for a possible parenteral dosage form." | ( Aqueous solvent system for the solubilization of azole compounds. Antal, I; Klebovich, I; Kovács, K; Ludányi, K; Stampf, G, 2009) | 0.58 |
| " Data collected from each record included signalment, clinical signs, results of ACTH stimulation tests before and after treatment with ketoconazole, serum alkaline phosphatase (ALP) and alanine aminotransferase (ALT) activities, dosage of ketoconazole, clinical response, and survival time." | ( Use of ketoconazole to treat dogs with pituitary-dependent hyperadrenocorticism: 48 cases (1994-2007). Huang, HP; Lien, YH, 2008) | 1 |
| " The bioassay was applied for a dose-response study of mono(2-ethylhexyl)phthalate (MEHP), a chemical known to disrupt several steroidogenic enzymes." | ( Steroidogenesis-disrupting compounds can be effectively studied for major fertility-related endpoints using in vitro cultured mouse follicles. Lenie, S; Smitz, J, 2009) | 0.35 |
| " For substrates with t(1/2) longer than that of KTZ, multiple KTZ dosing is critical and BID200 appears to provide greater inhibition than QD400." | ( Quantitative evaluation of pharmacokinetic inhibition of CYP3A substrates by ketoconazole: a simulation study. Huang, SM; Levy, RH; Ragueneau-Majlessi, I; Reynolds, KS; Strong, JM; Thummel, KE; Zhang, L; Zhao, P, 2009) | 0.58 |
| "Fesoterodine dosage should not exceed 4 mg once daily when taken concomitantly with potent CYP3A4 inhibitors." | ( Evaluation of drug-drug interactions with fesoterodine. Malhotra, B; Sachse, R; Wood, N, 2009) | 0.35 |
| " We used ketoconazole and prednisone with dosing titrated according to serum testosterone levels to suppress sleep related erections in an attempt to prevent recurrent episodes." | ( Ketoconazole and prednisone to prevent recurrent ischemic priapism. Abern, MR; Levine, LA, 2009) | 2.21 |
| " Testosterone was measured on initial presentation, and ketoconazole and prednisone dosing was titrated to approximately 200 ng/dl testosterone and based on the presence or absence of recurrent ischemic priapism episodes." | ( Ketoconazole and prednisone to prevent recurrent ischemic priapism. Abern, MR; Levine, LA, 2009) | 2.04 |
| "hr/ml (157%), respectively, after dosing with 10 mg loratadine tablets for 10 days." | ( Metabolism of loratadine and further characterization of its in vitro metabolites. Alton, KB; Alvarez, N; Chowdhury, SK; Ghosal, A; Gupta, S; Lu, X; Ramanathan, R; Su, AD; Yuan, Y; Zbaida, S, 2009) | 0.35 |
| " Protocols to reverse nephrotoxicity incorporate dosage reduction or withdrawal of these agents." | ( Two-year experience with tacrolimus in renal transplantation after late conversion from cyclosporine therapy. Videla, CO, ) | 0.13 |
| " Cyclosporine C0 or C2 levels and CsA dosage had previously been changed simultaneously with ketoconazole." | ( Two-year experience with tacrolimus in renal transplantation after late conversion from cyclosporine therapy. Videla, CO, ) | 0.35 |
| " Segment 2 was designed to evaluate the safety of dasatinib as dosing was increased." | ( Phase 1 pharmacokinetic and drug-interaction study of dasatinib in patients with advanced solid tumors. Agrawal, S; Blackwood-Chirchir, A; Burris, H; Chiappori, AA; Dhillon, N; Hong, D; Johnson, FM; Kaul, S; Luo, FR; Rosen, L; Sy, O, 2010) | 0.36 |
| " Serial blood samples were collected over the day-8 dosing interval (immediately prior to bortezomib administration, and from 5 minutes to 72 hours after administration) in cycles 1 and 2 for measurement of plasma bortezomib concentrations for noncompartmental PK analysis and blood 20S proteasome inhibition for PD analysis." | ( Effect of the CYP3A inhibitor ketoconazole on the pharmacokinetics and pharmacodynamics of bortezomib in patients with advanced solid tumors: a prospective, multicenter, open-label, randomized, two-way crossover drug-drug interaction study. Chatta, G; Chen, E; Cooper, M; Egorin, M; Karol, M; Neuwirth, R; Rader, M; Ramalingam, S; Ramanathan, RK; Riordan, W; Trepicchio, W; Venkatakrishnan, K; von Moltke, L, 2009) | 0.64 |
| "An intravenous solution is a dosage forms intended for administration into the bloodstream." | ( Composition optimization and stability testing of a parenteral antifungal solution based on a ternary solvent system. Antal, I; Klebovich, I; Kovács, K; Ludányi, K; Stampf, G, 2010) | 0.36 |
| " On day 3 of ketoconazole treatment, a second 100 mg of udenafil was dosed concomitantly." | ( Effect of ketoconazole on the pharmacokinetics of udenafil in healthy Korean subjects. Cho, JY; Chung, YJ; Jang, IJ; Kim, BH; Kim, HS; Kim, TE; Shin, KH; Shin, SG; Yu, KS, 2010) | 1.13 |
| "19 when udenafil was dosed in the presence of ketoconazole." | ( Effect of ketoconazole on the pharmacokinetics of udenafil in healthy Korean subjects. Cho, JY; Chung, YJ; Jang, IJ; Kim, BH; Kim, HS; Kim, TE; Shin, KH; Shin, SG; Yu, KS, 2010) | 1.02 |
| " When coadministered with rifampin, area under the plasma concentration-time curve over the dosing interval and maximum concentration values for linezolid were reduced approximately 32% and 21%, respectively." | ( Unexpected effect of rifampin on the pharmacokinetics of linezolid: in silico and in vitro approaches to explain its mechanism. Damle, B; Fahmi, OA; Gandelman, K; Glue, P; Lian, K; Obach, RS; Zhu, T, 2011) | 0.37 |
| " These results indicate that concurrent use of strong CYP3A4 inducers or inhibitors may necessitate dosage adjustments of nilotinib and should be avoided when possible." | ( Effects of rifampin and ketoconazole on the pharmacokinetics of nilotinib in healthy participants. Galitz, L; Grouss, K; Harrell, R; Schran, H; Sethuraman, V; Smith, T; Tanaka, C; Yin, OQ, 2011) | 0.68 |
| "In this randomized, single-blind, two-way crossover study, 32 healthy volunteers received placebo, followed by a single 5-mg oral dose of axitinib, administered either alone or on the fourth day of dosing with oral ketoconazole (400 mg/day for 7 days)." | ( Effect of ketoconazole on the pharmacokinetics of axitinib in healthy volunteers. Garrett, M; Hee, B; Klamerus, KJ; Mount, J; Pithavala, YK; Rahavendran, SV; Sarapa, N; Selaru, P; Tong, W, 2012) | 0.97 |
| " This method has been applied to the determination of ketoconazole in various pharmaceutical dosage forms." | ( High-performance thin-layer chromatographic determination of ketoconazole in pharmaceutical formulations. Liawruangrath, B; Liawruangrath, S; Saysin, S, ) | 0.62 |
| " Concomitant dosing with ketoconazole increased the area under the plasma concentration-time curve for AZD0837 (by 99%) and for AR-H067637 (by 51%)." | ( Effects of ketoconazole on the in vivo biotransformation and hepatobiliary transport of the thrombin inhibitor AZD0837 in pigs. Bottner, P; Eriksson, UG; Knutson, L; Lennernäs, H; Lundahl, A; Matsson, EM; Palm, JE, 2011) | 1.06 |
| " Serial blood samples were collected over 24 h for the iv dosed groups." | ( The effect of increased lipoprotein levels on the pharmacokinetics of ketoconazole enantiomers in the rat. Brocks, DR; Hamdy, DA, 2011) | 0.6 |
| " • Ketoconazole was administered by oral route at a dose of 200 mg every 8 h continuous dosing until the onset of serious adverse events or disease progression." | ( Low dose of ketoconazole in patients with prostate adenocarcinoma resistant to pharmacological castration. Bajetta, E; Capone, F; Giganti, MO; Guadalupi, V; Mariani, L; Nicolai, N; Procopio, G; Salvioni, R; Valdagni, R, 2011) | 1.37 |
| " The first group was dosed orally with TCBZ at a dosage of 10mg/kg and KTZ at a dosage of 10mg/kg." | ( Enhancement of triclabendazole action in vivo against a triclabendazole-resistant isolate of Fasciola hepatica by co-treatment with ketoconazole. Alvarez, LI; Brennan, GP; Devine, C; Fairweather, I; Hoey, E; Lanusse, CE; Trudgett, A, 2011) | 0.57 |
| " The data suggest that dosing diltiazem XR for 2 days predicts the change in midazolam AUC as reliably as 5 days of XR dosing and 2 days of CR dosing." | ( Effect of different durations and formulations of diltiazem on the single-dose pharmacokinetics of midazolam: how long do we go? Bergman, AJ; Chodakewitz, J; Fraser, IP; Friedman, EJ; Larson, PJ; Li, CC; Stoch, SA; Wagner, JA; Wang, YH, 2011) | 0.37 |
| " Using plasma ALF concentrations and area under the curve (AUC), clearance, or single-point concentrations, both simultaneous and sequential dosing provided equivalent results and detected hepatic and intestinal CYP3A induction and inhibition." | ( Concurrent assessment of hepatic and intestinal cytochrome P450 3A activities using deuterated alfentanil. Blood, J; Buck, N; Kharasch, ED; Kim, T; London, A; Mach, RH; Vangveravong, S, 2011) | 0.37 |
| " We proposed a systematic classification scheme using FDA-approved drug labeling to assess the DILI potential of drugs, which yielded a benchmark dataset with 287 drugs representing a wide range of therapeutic categories and daily dosage amounts." | ( FDA-approved drug labeling for the study of drug-induced liver injury. Chen, M; Fang, H; Liu, Z; Shi, Q; Tong, W; Vijay, V, 2011) | 0.37 |
| " Considering the variability in exposure following enzyme inhibition and the fact that chronic dosing of panobinostat was not studied with CYP3A inhibitors, close monitoring of panobinostat-related adverse events is necessary." | ( Effect of ketoconazole-mediated CYP3A4 inhibition on clinical pharmacokinetics of panobinostat (LBH589), an orally active histone deacetylase inhibitor. Chen, LC; de Jonge, M; Hamberg, P; Hengelage, T; Li, W; Porro, MG; Sharma, S; van der Biessen, D; Verweij, J; Woo, MM; Zhao, L, 2011) | 0.77 |
| " For 12 weeks they were treated with neoadjuvant docetaxel and ketoconazole, with dosing based on phase I data." | ( A phase II clinical trial of neoadjuvant ketoconazole and docetaxel chemotherapy before radical prostatectomy in high risk patients. Holzbeierlein, JM; Nisbet, AA; Reed, GA; Thrasher, JB; VanVeldhuizen, PJ; Womble, PR, 2011) | 0.87 |
| " hepatica, dosed orally with triclabendazole at a dosage of 10mg/kg live weight and ketoconazole at a dosage of 10mg/kg live weight." | ( Potentiation of triclabendazole action in vivo against a triclabendazole-resistant isolate of Fasciola hepatica following its co-administration with the metabolic inhibitor, ketoconazole. Alvarez, LI; Brennan, GP; Devine, C; Fairweather, I; Hoey, E; Lanusse, CE; Trudgett, A, 2012) | 0.8 |
| " Here we present the results in the relief of vaginitis and vaginosis with two different dosage forms." | ( [Evaluation of efficacy of ketoconazole 800 mg-clindamycin 100 mg tablets vaginal against ketoconazole 800 mg- clindamycin 100 mg vaginal capsules in candida vaginitis and vaginosis]. Bravo-Topete, EG; Cejudo-Alvarez, J; Garibay-Valencia, M; Herrera-Villalobos, JE; Martínez-García, A; Mirabent-González, F, 2011) | 0.67 |
| " As tolvaptan is a CYP3A4 substrate, knowing the effects of inhibition and induction on CYP3A4-mediated metabolism was important for dosing recommendations." | ( Effects of CYP3A4 inhibition and induction on the pharmacokinetics and pharmacodynamics of tolvaptan, a non-peptide AVP antagonist in healthy subjects. Bricmont, P; Mallikaarjun, S; Shoaf, SE, 2012) | 0.38 |
| " In this study, we quantified the inhibitory activity and specificity of orteronel for testicular and adrenal androgen production by evaluating its effects on CYP17A1 enzymatic activity, steroid production in monkey adrenal cells and human adrenal tumor cells, and serum levels of dehydroepiandrosterone (DHEA), cortisol, and testosterone after oral dosing in castrated and intact male cynomolgus monkeys." | ( Orteronel (TAK-700), a novel non-steroidal 17,20-lyase inhibitor: effects on steroid synthesis in human and monkey adrenal cells and serum steroid levels in cynomolgus monkeys. Asahi, S; Hara, T; Hitaka, T; Kaku, T; Kusaka, M; Miki, H; Takahashi, J; Takeuchi, T; Tasaka, A; Yamaoka, M, 2012) | 0.38 |
| "The conventional dosage form of Ketoconazole (KZ) shows poor absorption due to rapid gastric emptying." | ( Chitosan based mucoadhesive nanoparticles of ketoconazole for bioavailability enhancement: formulation, optimization, in vitro and ex vivo evaluation. Joshi, G; Modi, J; Sawant, K, 2013) | 0.93 |
| " Repeated dosing of LB42908 in rats did not significantly affect its own metabolism, indicating that long-term administration of LB42908 would not alter its pharmacokinetic profiles." | ( Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities. Aeri, K; Chang, M; Kim, HJ; Koh, JS; Lee, SH, 2012) | 0.38 |
| " The exploration of the intestinal absorption mechanism is crucial to the design of dosage form and clinical use of limonin." | ( [Transport of limonin in rat intestine in situ and Caco-2 cells in vitro]. He, L; Ke, X; Tian, JL; Zhang, XY, 2012) | 0.38 |
| " Depending on the dosage form administered in in vivo studies, a solution or a suspension was placed in the gastric compartment." | ( An in vitro methodology for forecasting luminal concentrations and precipitation of highly permeable lipophilic weak bases in the fasted upper small intestine. Busby, D; Butler, J; Dressman, J; Psachoulias, D; Reppas, C; Symillides, M; Vertzoni, M, 2012) | 0.38 |
| " The absence of stereoselectivity after iv dosing indicates that the first-pass tissue binding effect is an important factor in determining the steroselective PK of R/S-VER after oral administration." | ( Binding processes determine the stereoselective intestinal and hepatic extraction of verapamil in vivo. Dickinson, PA; Lennernäs, H; Sjögren, E; Thörn, HA, 2012) | 0.38 |
| " The extract was as effective as the positive control ketoconazole dosed at 60 mg/kg." | ( A controlled study to determine the efficacy of Loxostylis alata (Anacardiaceae) in the treatment of aspergillus in a chicken (Gallus domesticus) model in comparison to ketoconazole. Duncan, N; Eloff, JN; Naidoo, V; Suleiman, MM, 2012) | 0.82 |
| "5]octan-6-yl] N-[(2R)-1-amino-3-methyl-1-oxobutan-2-yl]carbamate, demonstrates rapid inactivation of its molecular target, methionine aminopeptidase-2 (MetAP2), and good efficacy in several rodent models of cancer and inflammation with oral dosing despite low apparent oral bioavailability." | ( Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. Arico-Muendel, CC; Belanger, B; Benjamin, D; Blanchette, HS; Caiazzo, TM; Centrella, PA; DeLorey, J; Doyle, EG; Gradhand, U; Griffin, ST; Hill, S; Labenski, MT; Morgan, BA; O'Donovan, G; Prasad, K; Skinner, S; Taghizadeh, N; Thompson, CD; Wakefield, J; Westlin, W; White, KF, 2013) | 0.39 |
| " Dose-response curves were obtained for the correlation between hormone concentrations and the concentration of the individual disruptors." | ( Corticosteroid production in H295R cells during exposure to 3 endocrine disrupters analyzed with LC-MS/MS. Hansen, M; Nielsen, FK; Styrishave, B; Winther, CS, ) | 0.13 |
| " Steady-state mirabegron pharmacokinetic parameters (50 and 100 mg mirabegron OCAS) were similar in 13 CYP2D6 poor, 40 intermediate, and 99 extensive metabolizers, whereas C max and AUC under the dosing interval τ of 24 h (AUCτ) were 30-47 % lower in 10 ultrarapid metabolizers." | ( Role of cytochrome p450 isoenzymes 3A and 2D6 in the in vivo metabolism of mirabegron, a β3-adrenoceptor agonist. Keirns, J; Kerbusch, V; Kowalski, D; Krauwinkel, W; Lee, J; Marion, A; Meijer, J; Moy, S; Roy, M; Sawamoto, T; Takusagawa, S; van Gelderen, M, 2013) | 0.39 |
| " Alternative dosing regimens that do not increase gastric pH at the time of pazopanib dosing should be considered." | ( Effects of ketoconazole and esomeprazole on the pharmacokinetics of pazopanib in patients with solid tumors. Botbyl, J; Edenfield, JW; Gibbon, DG; Gregory, C; Lindquist, D; Martin, JC; Stein, MN; Stephenson, JJ; Suttle, AB; Tada, H; Tan, AR, 2013) | 0.78 |
| " Study treatments were administered orally for 3 days in five separate periods in which subjects were dosed with (1) a single dose of 75 mg lomitapide on Day 1 followed by a single dose of 200 mg on Day 3; (2) ketoconazole 200 mg BID; (3) ketoconazole with a single dose of 75 mg lomitapide on Day 3; (4) a single dose of 400 mg moxifloxacin on Day 3 and (5) placebo." | ( Lomitapide at supratherapeutic plasma levels does not prolong the Qtc interval--results from a TQT study with moxifloxacin and ketoconazole. Darpo, B; Ferber, G; Sager, P; Sumeray, M; Zhou, M, 2013) | 0.78 |
| " Each subject received the following 2 treatments in a randomly allocated sequence, separated by a washout period of 42 days: single oral dose of CG100649 6 mg, and concurrent dosing of CG100649 6 mg and ketoconazole 400 mg followed by ketoconazole 400 mg/d over 4 days." | ( Effects of ketoconazole on the pharmacokinetic properties of CG100649, a novel NSAID: a randomized, open-label crossover study in healthy Korean male volunteers. Bae, KS; Jin, SJ; Jung, JA; Kim, UJ; Ko, YJ; Lim, HS; Noh, YH; Youn Choi, H, 2014) | 0.98 |
| " We compared our previous protocol of three times daily (TID) KTZ dosing with prednisone for 6 months with our current regimen of initiating KTZ 200 mg TID with prednisone 5 mg daily for 2 weeks and then tapering to KTZ 200 mg nightly for 6 months." | ( Prevention of recurrent ischemic priapism with ketoconazole: evolution of a treatment protocol and patient outcomes. Hoeh, MP; Levine, LA, 2014) | 0.66 |
| "Seven phase I studies were conducted to investigate the effects of repeated dosing of ketoconazole, diltiazem, rifampin, or lithium on the pharmacokinetics (PK) of single oral doses of lurasidone, or the effects of repeated dosing of lurasidone on the PK of digoxin, midazolam, or the oral contraceptive norgestimate/ethinyl estradiol." | ( Lurasidone drug-drug interaction studies: a comprehensive review. Chiu, YY; Ereshefsky, L; Loebel, A; Poola, N; Preskorn, SH, 2014) | 0.63 |
| " Steady-state dosing with lurasidone increased Cmax and AUC0-24 (AUC from time 0 to 24 h postdose) of digoxin by 9% and 13%, respectively, and of midazolam by 21% and 44%, respectively." | ( Lurasidone drug-drug interaction studies: a comprehensive review. Chiu, YY; Ereshefsky, L; Loebel, A; Poola, N; Preskorn, SH, 2014) | 0.4 |
| "Lurasidone PK is altered by strong cytochrome P450 (CYP) 3A4 inhibitors or inducers, and coadministration is contraindicated; whereas moderate CYP3A4 inhibitors have less effect, and lurasidone dosage restrictions are recommended." | ( Lurasidone drug-drug interaction studies: a comprehensive review. Chiu, YY; Ereshefsky, L; Loebel, A; Poola, N; Preskorn, SH, 2014) | 0.4 |
| "These results suggest that up to a 50% decrease of vilazodone dosage should be considered when it is given in combination with strong CYP3A4 inhibitors; conversely, increasing the vilazodone dosage up to a maximum of 80 mg/d should be considered when it is given in combination with strong CYP3A4 inducers." | ( Influence of CYP3A4 induction/inhibition on the pharmacokinetics of vilazodone in healthy subjects. Boinpally, R; Gad, N; Gupta, S; Periclou, A, 2014) | 0.4 |
| "The aim of the study was to assess the magnitude of the CYP3A4 inhibitory effect of 2 dosing regimens of ketoconazole and the influence of the pharmacokinetic properties of the CYP3A4 substrate on the extent of the substrate exposure increase." | ( CYP3A4-based drug-drug interaction: CYP3A4 substrates' pharmacokinetic properties and ketoconazole dose regimen effect. Boulenc, X; Donazzolo, Y; Hermabessière, S; Martin, V; Nicolas, O; Ollier, C; Zobouyan, I, 2016) | 0.87 |
| " Clinically fentanyl dosage adjustments may become necessary when ketoconazole or other strong CYP3A inhibitors are given simultaneously." | ( Pharmacokinetic interaction of intravenous fentanyl with ketoconazole. Haefeli, WE; König, SK; Mahlke, NS; Mikus, G; Skopp, G; Ziesenitz, VC, 2015) | 0.9 |
| " RAUC values were not significantly related to inhibitor dosage or to duration of inhibitor pre-exposure prior to administration of MDZ." | ( Ritonavir is the best alternative to ketoconazole as an index inhibitor of cytochrome P450-3A in drug-drug interaction studies. Greenblatt, DJ; Harmatz, JS, 2015) | 0.69 |
| " Various factors considered in the recommendations include the choice of itraconazole dosage form, administration in the fasted or fed state, the dose and duration of itraconazole administration, the timing of substrate and itraconazole coadministration, and measurement of itraconazole and metabolite plasma concentrations, among others." | ( Best practices for the use of itraconazole as a replacement for ketoconazole in drug-drug interaction studies. Bello, A; Dresser, MJ; Heald, D; Komjathy, SF; Liu, L; O'Mara, E; Robertson, SM; Rogge, M; Stoch, SA, 2016) | 0.67 |
| " The impact of HAART on imatinib may depend on whether it is being initiated or has already been dosed chronically in patients." | ( Human hepatocyte assessment of imatinib drug-drug interactions - complexities in clinical translation. Beumer, JH; Christner, SM; Kiesel, BF; Parise, RA; Pillai, VC; Rudek, MA; Venkataramanan, R, 2015) | 0.42 |
| " The model was robust enough to allow prospective predictions of macitentan-drug combinations not studied, including an alternative dosing regimen of ketoconazole and nine other CYP3A4-interacting drugs." | ( Physiologically-Based Pharmacokinetic Modeling of Macitentan: Prediction of Drug-Drug Interactions. Buchmann, S; de Kanter, R; Delahaye, S; Gnerre, C; Kohl, C; Segrestaa, J; Sidharta, PN; Treiber, A, 2016) | 0.63 |
| " For example, the accuracy and the precision of the method were determined by a recovery study at 80, 100 and 120% of the tablet dosage levels." | ( Development and Validation of Stability-Indicating Method for the Simultaneous Determination of Ketoconazole and Beauvericin in Pharmaceutical Tablets. Liu, Y; Luan, Y; Tang, X; Tian, T; Yang, M; Zhao, Z; Zhu, M, 2016) | 0.65 |
| "BioGIT system could be useful for the evaluation of the impact of gastrointestinal transfer on concentrations in the upper intestinal lumen during the first hour, after oral administration of dispersing/solution dosage forms of lipophilic weak bases." | ( An in vitro biorelevant gastrointestinal transfer (BioGIT) system for forecasting concentrations in the fasted upper small intestine: Design, implementation, and evaluation. Augustijns, P; Brouwers, J; Kourentas, A; Reppas, C; Stavrinoudakis, N; Symillides, M; Symillidis, A; Vertzoni, M, 2016) | 0.43 |
| " For this purpose, we measured plasma concentrations of adrenal steroids in rats dosed with ketoconazole, a known inhibitor of adrenal steroidogenesis, and examined its relationship with the changes in histopathology and mRNA expression of steroidogenic enzymes in the adrenal gland." | ( Changes in plasma concentrations of corticosterone and its precursors after ketoconazole administration in rats: An application of simultaneous measurement of multiple steroids using LC-MS/MS. Fujii, Y; Funabashi, H; Kouchi, M; Matsumoto, I; Miyawaki, I; Tochitani, T; Yamada, T; Yamashita, A, ) | 0.58 |
| "Although using spray-dried dispersions (SDDs) to improve the bioavailability of poorly water-soluble compounds has become a common practice in supporting the early phases of clinical studies, their performance evaluation, whether in solid dosage forms or alone, still presents significant challenges." | ( Evaluation of the Microcentrifuge Dissolution Method as a Tool for Spray-Dried Dispersion. Li, J; Wang, Y; Wu, B, 2016) | 0.43 |
| " Steady-state ketoconazole did not cause a clinically significant change in the pharmacokinetics of a single dose of tivozanib; therefore, dosing of tivozanib with a CYP3A4 pathway inhibitor should not cause a clinically significant change in serum tivozanib levels." | ( Effects of ketoconazole or rifampin on the pharmacokinetics of tivozanib hydrochloride, a vascular endothelial growth factor receptor tyrosine kinase inhibitor. Cotreau, MM; Miller, J; Siebers, NM; Slichenmyer, W; Strahs, AL, 2015) | 1.17 |
| " The aim of this study was to evaluate whether the oral absorption of 2 poorly soluble, weakly basic APIs, ketoconazole (KETO) and posaconazole (POSA), would be equally sensitive to changes in dissolution rate under the following dosing conditions-coadministration with water, with food, with carbonated drinks, and in drug-induced hypochlorhydria." | ( Assessment of Bioequivalence of Weak Base Formulations Under Various Dosing Conditions Using Physiologically Based Pharmacokinetic Simulations in Virtual Populations. Case Examples: Ketoconazole and Posaconazole. Cristofoletti, R; Dressman, JB; Patel, N, 2017) | 0.86 |
| "The impact of different single oral doses of ketoconazole (KTZ) (100, 200 and 400 mg) and of staggering its dosage (400 mg at -12, -2, 0, 2 and 4 h), with respect to the administration of a single 5 mg oral dose of midazolam (MDZ) on the extent of inhibition of the metabolism of the latter, was evaluated in healthy subjects in two separate studies." | ( The absorption kinetics of ketoconazole plays a major role in explaining the reported variability in the level of interaction with midazolam: Interplay between formulation and inhibition of gut wall and liver metabolism. Crewe, HK; Liu, B; Ozdemir, M; Rostami-Hodjegan, A; Rowland Yeo, K; Tucker, G, 2017) | 1.01 |
| " The Gastrointestinal Simulator (GIS) consists of three compartments, the gastric, duodenal and jejunal chambers, and is a practical in vitro dissolution apparatus to predict in vivo dissolution for oral dosage forms." | ( The impact of supersaturation level for oral absorption of BCS class IIb drugs, dipyridamole and ketoconazole, using in vivo predictive dissolution system: Gastrointestinal Simulator (GIS). Amidon, GE; Amidon, GL; Matsui, K; Searls, AL; Sun, D; Takeuchi, S; Tsume, Y, 2017) | 0.67 |
| " We have now determined the effects of concurrent ketoconazole on 4-HPR cytotoxic dose-response in four neuroblastoma (NB) cell lines in vitro and on 4-HPR activity against two cell line-derived, subcutaneous NB xenografts (CDX) and three patient-derived NB xenografts (PDX)." | ( P450 inhibitor ketoconazole increased the intratumor drug levels and antitumor activity of fenretinide in human neuroblastoma xenograft models. Kang, MH; Lopez-Barcons, L; Maurer, BJ; Reynolds, CP, 2017) | 1.06 |
| " Following dose-response screening of 25 strains, 4 were selected on the basis of resistance or sensitivity relative to the standard laboratory strain BY." | ( The genetic architecture in Saccharomyces cerevisiae that contributes to variation in drug response to the antifungals benomyl and ketoconazole. Atkinson, PH; Miller, JH; Roberts, CA, 2017) | 0.66 |
| "To clarify the molecular mechanism of ethylene glycol monomethyl ether (EGME)-induced testicular toxicity, the potential for EGME-related changes in transcript levels of genes including spermatocyte-specific genes was evaluated in the testis of rats given single dosing of EGME at 200, 600, or 2000 mg/kg." | ( Transcriptional profile of ethylene glycol monomethyl ether-induced testicular toxicity in rats. Ando, Y; Iida, H; Ito, K; Kuwata, C; Matsuyama, T; Mori, K; Yabe, K, 2018) | 0.48 |
| " To conclude, tramadol and M1 concentrations were low and variable in dogs after oral dosing of tramadol, even in combination with cimetidine or ketoconazole, but effective concentrations in dogs have not been defined." | ( The effects of ketoconazole and cimetidine on the pharmacokinetics of oral tramadol in greyhound dogs. Black, J; KuKanich, B; KuKanich, K, 2017) | 1.01 |
| " Moreover, our results point out the need for future in vivo studies to confirm the nature of ketoconazole-antimony interaction and also to determine possible effective dosage regimens related to ketoconazole administration in association with the optimal lower dose of antimony." | ( In vitro additive interaction between ketoconazole and antimony against intramacrophage Leishmania (Leishmania) amazonensis amastigotes. Bispo-da-Silva, LB; Costa, MS; Figueira, MMNR; Napolitano, DR; Nunes, DCO; Rodrigues, RS; Rodrigues, VM; Yoneyama, KAG, 2017) | 0.95 |
| " Although the lack of a dose-response effect in the synergistic bioassay warrants further exploration, our study may have broad implications for the control of parasitic and vector-borne diseases." | ( Cytochrome P450/ABC transporter inhibition simultaneously enhances ivermectin pharmacokinetics in the mammal host and pharmacodynamics in Anopheles gambiae. Abizanda, G; Aldaz, A; Alustiza, M; Bilbao, JI; Castejon, S; Chaccour, CJ; Del Pozo, JL; Hammann, F; Irigoyen Barrio, Á; Maia, M; Martí Soler, H; Moncada, R; Tarimo, BB, 2017) | 0.46 |
| " Therefore, this new formulation could prove to be a novel ocular dosage form able to prolong the residence time and to control the release of drug when administered into the eye." | ( A novel thermo-sensitive hydrogel-based on poly(N-isopropylacrylamide)/hyaluronic acid of ketoconazole for ophthalmic delivery. Li, N; Wang, J; Zhu, M, 2018) | 0.7 |
| " This study attempted the formulation of stable, double fixed-dose acyclovir and ketoconazole novel transmucosal dosage forms, which are able to provide an efficient flux for both compounds." | ( Formulation and evaluation of selected transmucosal dosage forms containing a double fixed-dose of acyclovir and ketoconazole. Botes, D; Steenekamp, JH; Viljoen, JM, 2018) | 0.92 |
| "2 observed ratio) after daily dosing of midostaurin for 4 days." | ( Simultaneous Physiologically Based Pharmacokinetic (PBPK) Modeling of Parent and Active Metabolites to Investigate Complex CYP3A4 Drug-Drug Interaction Potential: A Case Example of Midostaurin. Chun, DY; Dutreix, C; Einolf, HJ; Gu, H; He, H; Ouatas, T; Rebello, S; Wang, L, 2018) | 0.48 |
| "Current dosing regimens of reported drugs are effective and safe for use in tinea capitis in children." | ( Tinea capitis in children: a systematic review of management. Friedlander, SF; Gupta, AK; Mays, RR; Piguet, V; Piraccini, BM; Shear, NH; Tosti, A; Versteeg, SG, 2018) | 0.48 |
| "Physicochemical properties of the hexosomes containing ketoconazole are important for topical mycosis treatment administration, conditions of storage, and for its incorporation into the formulation of semi-solid dosage forms." | ( Physicochemical characterization and thermal behavior of hexosomes containing ketoconazole as potential topical antifungal delivery system. Angélica Noguez-Méndez, N; Faustino-Vega, A; Gazga-Urioste, C; Pérez-Hernández, G; Rivera-Becerril, E; Tomás Quirino-Barreda, C, 2019) | 0.99 |
| " Therefore, in silico approaches are a potential tool to assess a pharmaceutical product's performance and efficacy under different physiological and pathophysiological states supporting the assessment of different dosing strategies in clinical practice." | ( Application of in Silico Tools in Clinical Practice using Ketoconazole as a Model Drug. Davies, NM; Duque, MD; Ferraz, HG; Löbenberg, R; Silva, DA, 2018) | 0.73 |
| " Therefore, although dosed as DABE, a P-gp drug-drug interaction (DDI) is reported as a dabigatran plasma concentration ratio (perpetrator versus placebo)." | ( Renal Excretion of Dabigatran: The Potential Role of Multidrug and Toxin Extrusion (MATE) Proteins. Marathe, P; Rodrigues, AD; Shen, H; Sinz, M; Yao, M; Zhu, M, 2019) | 0.51 |
| "To verify simultaneous measurement of blood levels of adrenal steroids as a tool to evaluate drug effects on adrenal steroidogenesis, dose- and time-dependent changes in blood levels of corticosterone and its precursors (pregnenolone, progesterone and deoxycorticosterone), as well as their relationship with the pathological changes in the adrenal gland, were examined in rats dosed with ketoconazole (KET)." | ( Dose- and time-dependent changes in blood and adrenal levels of multiple steroids in rats after administration of ketoconazole with or without ACTH. Fujii, Y; Kouchi, M; Matsumoto, I; Miyawaki, I; Tochitani, T; Yamashita, A, 2019) | 0.89 |
| " The combination of ketoconazole-CNIs can reduce the cost of medication for patients by reducing the dosage of CNIs, but its safety is still controversial." | ( Efficacy and safety of ketoconazole combined with calmodulin inhibitor in solid organ transplantation: A systematic review and meta-analysis. Chen, C; Cui, Y; Li, M; Ma, L; Wu, S; Xue, T; Yang, T; Zhou, Y, 2020) | 1.19 |
| "Commercial development of nanosuspensions for oral drug delivery generally involves a drying step which aims to generate a stable product that rapidly releases the nanocrystals once rehydrated and can be easily processed into a final dosage form (e." | ( Formulation of Ketoconazole Nanocrystal-Based Cryopellets. Lamprecht, A; Pellequer, Y; Pfefferlé, F; Touzet, A, 2020) | 0.91 |
| " The current PBPK model, which considers changes in unbound potency-adjusted active species, can be used to inform dosing recommendations when abemaciclib is coadministered with CYP3A4 perpetrators." | ( Predicting Clinical Effects of CYP3A4 Modulators on Abemaciclib and Active Metabolites Exposure Using Physiologically Based Pharmacokinetic Modeling. Dickinson, GL; Hall, SD; Kulanthaivel, P; Morse, BL; Posada, MM; Turner, PK, 2020) | 0.56 |
| "In vitro dissolution tests are widely used to monitor the quality and consistency of oral solid dosage forms, but to increase the physiological relevance of in vitro dissolution tests, newer systems combine dissolution and permeation measurements." | ( A differential equation based modelling approach to predict supersaturation and in vivo absorption from in vitro dissolution-absorption system (idas2) data. Bermejo, M; Gonzalez-Alvarez, I; Hidalgo, IJ; Li, J; Silchenko, S; Spivey, N, 2021) | 0.62 |
| Class | Description |
|---|---|
| cis-1-acetyl-4-(4-{[2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy}phenyl)piperazine | Either of the two diastereoisomers of 1-acetyl-4-(4-{[2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy}phenyl)piperazine in which the imidazol-1-ylmethyl group and the aryloxymethyl group are in a cis relationship to each other - i.e. they are both on the same side of the plane of the dioxolane ring. The antifungal drug ketoconazole is a racemic mixture of the two cis diastereoisomers. |
| ether | An organooxygen compound with formula ROR, where R is not hydrogen. |
| imidazoles | A five-membered organic heterocycle containing two nitrogen atoms at positions 1 and 3, or any of its derivatives; compounds containing an imidazole skeleton. |
| N-arylpiperazine | |
| dioxolane | |
| dichlorobenzene | Any member of the class of chlorobenzenes carrying two chloro groups at unspecified positions. |
| N-acylpiperazine | |
| [compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Chain A, TYROSYL-DNA PHOSPHODIESTERASE | Homo sapiens (human) | Potency | 45.3736 | 0.0040 | 23.8416 | 100.0000 | AID485290 |
| Chain A, Beta-lactamase | Escherichia coli K-12 | Potency | 11.9047 | 0.0447 | 17.8581 | 100.0000 | AID485341 |
| Chain A, JmjC domain-containing histone demethylation protein 3A | Homo sapiens (human) | Potency | 30.3001 | 0.6310 | 35.7641 | 100.0000 | AID504339 |
| Chain A, Cruzipain | Trypanosoma cruzi | Potency | 39.8107 | 0.0020 | 14.6779 | 39.8107 | AID1476 |
| acetylcholinesterase | Homo sapiens (human) | Potency | 33.6398 | 0.0025 | 41.7960 | 15,848.9004 | AID1347395; AID1347398 |
| glp-1 receptor, partial | Homo sapiens (human) | Potency | 17.7828 | 0.0184 | 6.8060 | 14.1254 | AID624417 |
| thioredoxin reductase | Rattus norvegicus (Norway rat) | Potency | 23.7781 | 0.1000 | 20.8793 | 79.4328 | AID588453 |
| hypoxia-inducible factor 1 alpha subunit | Homo sapiens (human) | Potency | 50.4169 | 3.1890 | 29.8841 | 59.4836 | AID1224846; AID1224894 |
| RAR-related orphan receptor gamma | Mus musculus (house mouse) | Potency | 10.4922 | 0.0060 | 38.0041 | 19,952.5996 | AID1159521; AID1159523 |
| SMAD family member 2 | Homo sapiens (human) | Potency | 54.9410 | 0.1737 | 34.3047 | 61.8120 | AID1346924 |
| ATAD5 protein, partial | Homo sapiens (human) | Potency | 13.7087 | 0.0041 | 10.8903 | 31.5287 | AID493106; AID493107; AID504467 |
| Fumarate hydratase | Homo sapiens (human) | Potency | 32.5236 | 0.0030 | 8.7949 | 48.0869 | AID1347053 |
| USP1 protein, partial | Homo sapiens (human) | Potency | 44.6684 | 0.0316 | 37.5844 | 354.8130 | AID504865 |
| NFKB1 protein, partial | Homo sapiens (human) | Potency | 5.6234 | 0.0282 | 7.0559 | 15.8489 | AID895; AID928 |
| SMAD family member 3 | Homo sapiens (human) | Potency | 54.9410 | 0.1737 | 34.3047 | 61.8120 | AID1346924 |
| TDP1 protein | Homo sapiens (human) | Potency | 14.2234 | 0.0008 | 11.3822 | 44.6684 | AID686978; AID686979 |
| GLI family zinc finger 3 | Homo sapiens (human) | Potency | 27.4854 | 0.0007 | 14.5928 | 83.7951 | AID1259368; AID1259369; AID1259392 |
| Microtubule-associated protein tau | Homo sapiens (human) | Potency | 16.7074 | 0.1800 | 13.5574 | 39.8107 | AID1460 |
| Thrombopoietin | Homo sapiens (human) | Potency | 12.5893 | 0.0251 | 7.3048 | 31.6228 | AID917; AID918 |
| AR protein | Homo sapiens (human) | Potency | 19.6030 | 0.0002 | 21.2231 | 8,912.5098 | AID1259243; AID1259247; AID743035; AID743036; AID743042; AID743053; AID743054; AID743063 |
| Smad3 | Homo sapiens (human) | Potency | 14.9871 | 0.0052 | 7.8098 | 29.0929 | AID588855 |
| caspase 7, apoptosis-related cysteine protease | Homo sapiens (human) | Potency | 68.5896 | 0.0133 | 26.9810 | 70.7614 | AID1346978 |
| aldehyde dehydrogenase 1 family, member A1 | Homo sapiens (human) | Potency | 39.8107 | 0.0112 | 12.4002 | 100.0000 | AID1030 |
| thyroid stimulating hormone receptor | Homo sapiens (human) | Potency | 39.8107 | 0.0013 | 18.0743 | 39.8107 | AID926 |
| estrogen receptor 2 (ER beta) | Homo sapiens (human) | Potency | 21.6899 | 0.0006 | 57.9133 | 22,387.1992 | AID1259377; AID1259378 |
| nuclear receptor subfamily 1, group I, member 3 | Homo sapiens (human) | Potency | 9.1938 | 0.0010 | 22.6508 | 76.6163 | AID1224838; AID1224839; AID1224893 |
| progesterone receptor | Homo sapiens (human) | Potency | 7.6105 | 0.0004 | 17.9460 | 75.1148 | AID1346784; AID1346795 |
| regulator of G-protein signaling 4 | Homo sapiens (human) | Potency | 37.6858 | 0.5318 | 15.4358 | 37.6858 | AID504845 |
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 0.1068 | 0.0123 | 7.9835 | 43.2770 | AID1645841 |
| EWS/FLI fusion protein | Homo sapiens (human) | Potency | 19.9242 | 0.0013 | 10.1577 | 42.8575 | AID1259252; AID1259253; AID1259255; AID1259256 |
| nonstructural protein 1 | Influenza A virus (A/WSN/1933(H1N1)) | Potency | 3.5481 | 0.2818 | 9.7212 | 35.4813 | AID2326 |
| glucocorticoid receptor [Homo sapiens] | Homo sapiens (human) | Potency | 52.2599 | 0.0002 | 14.3764 | 60.0339 | AID720691; AID720692; AID720719 |
| retinoic acid nuclear receptor alpha variant 1 | Homo sapiens (human) | Potency | 67.7531 | 0.0030 | 41.6115 | 22,387.1992 | AID1159552; AID1159553; AID1159555 |
| retinoid X nuclear receptor alpha | Homo sapiens (human) | Potency | 37.1228 | 0.0008 | 17.5051 | 59.3239 | AID1159527; AID1159531; AID588544; AID588546 |
| estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 18.1872 | 0.0015 | 30.6073 | 15,848.9004 | AID1224819; AID1224820; AID1224821; AID1224841; AID1224842; AID1224848; AID1224849; AID1259401; AID1259403 |
| farnesoid X nuclear receptor | Homo sapiens (human) | Potency | 37.6169 | 0.3758 | 27.4851 | 61.6524 | AID588526; AID743217; AID743220 |
| pregnane X nuclear receptor | Homo sapiens (human) | Potency | 68.5896 | 0.0054 | 28.0263 | 1,258.9301 | AID1346982 |
| estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 26.0151 | 0.0002 | 29.3054 | 16,493.5996 | AID1259244; AID1259248; AID588513; AID743069; AID743075; AID743077; AID743078; AID743079; AID743080; AID743091 |
| G | Vesicular stomatitis virus | Potency | 5.3547 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| cytochrome P450 2D6 | Homo sapiens (human) | Potency | 16.9330 | 0.0010 | 8.3798 | 61.1304 | AID1645840 |
| polyprotein | Zika virus | Potency | 32.5236 | 0.0030 | 8.7949 | 48.0869 | AID1347053 |
| bromodomain adjacent to zinc finger domain 2B | Homo sapiens (human) | Potency | 26.6321 | 0.7079 | 36.9043 | 89.1251 | AID504333 |
| peroxisome proliferator-activated receptor delta | Homo sapiens (human) | Potency | 61.6448 | 0.0010 | 24.5048 | 61.6448 | AID743227 |
| peroxisome proliferator activated receptor gamma | Homo sapiens (human) | Potency | 42.4019 | 0.0010 | 19.4141 | 70.9645 | AID588536; AID588537; AID743094; AID743140; AID743191 |
| vitamin D (1,25- dihydroxyvitamin D3) receptor | Homo sapiens (human) | Potency | 39.3376 | 0.0237 | 23.2282 | 63.5986 | AID588541; AID743223; AID743241 |
| caspase-3 | Homo sapiens (human) | Potency | 68.5896 | 0.0133 | 26.9810 | 70.7614 | AID1346978 |
| euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 23.7321 | 0.0355 | 20.9770 | 89.1251 | AID504332 |
| aryl hydrocarbon receptor | Homo sapiens (human) | Potency | 11.8729 | 0.0007 | 23.0674 | 1,258.9301 | AID651777; AID743085; AID743122 |
| cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_a | Homo sapiens (human) | Potency | 30.6379 | 0.0017 | 23.8393 | 78.1014 | AID743083 |
| thyroid stimulating hormone receptor | Homo sapiens (human) | Potency | 50.6866 | 0.0016 | 28.0151 | 77.1139 | AID1224895; AID1259385; AID1259395 |
| activating transcription factor 6 | Homo sapiens (human) | Potency | 18.1216 | 0.1434 | 27.6121 | 59.8106 | AID1159516; AID1159519 |
| thyrotropin-releasing hormone receptor | Homo sapiens (human) | Potency | 37.9534 | 0.1549 | 17.8702 | 43.6557 | AID1346877 |
| nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_a | Homo sapiens (human) | Potency | 37.3725 | 19.7391 | 45.9784 | 64.9432 | AID1159509; AID1159518 |
| v-jun sarcoma virus 17 oncogene homolog (avian) | Homo sapiens (human) | Potency | 17.4891 | 0.0578 | 21.1097 | 61.2679 | AID1159526; AID1159528 |
| Histone H2A.x | Cricetulus griseus (Chinese hamster) | Potency | 50.4772 | 0.0391 | 47.5451 | 146.8240 | AID1224845 |
| Bloom syndrome protein isoform 1 | Homo sapiens (human) | Potency | 3.5481 | 0.5406 | 17.6392 | 96.1227 | AID2364; AID2528 |
| cytochrome P450 2D6 isoform 1 | Homo sapiens (human) | Potency | 25.1189 | 0.0020 | 7.5337 | 39.8107 | AID891 |
| peripheral myelin protein 22 isoform 1 | Homo sapiens (human) | Potency | 42.5615 | 23.9341 | 23.9341 | 23.9341 | AID1967 |
| cytochrome P450 2C19 precursor | Homo sapiens (human) | Potency | 12.5893 | 0.0025 | 5.8400 | 31.6228 | AID899 |
| cytochrome P450 2C9 precursor | Homo sapiens (human) | Potency | 12.5893 | 0.0063 | 6.9043 | 39.8107 | AID883 |
| D(1A) dopamine receptor | Homo sapiens (human) | Potency | 23.7359 | 0.0224 | 5.9449 | 22.3872 | AID488981; AID488983 |
| chromobox protein homolog 1 | Homo sapiens (human) | Potency | 32.4648 | 0.0060 | 26.1688 | 89.1251 | AID488953; AID540317 |
| nuclear factor erythroid 2-related factor 2 isoform 2 | Homo sapiens (human) | Potency | 17.3582 | 0.0041 | 9.9848 | 25.9290 | AID504444 |
| potassium voltage-gated channel subfamily H member 2 isoform d | Homo sapiens (human) | Potency | 23.7359 | 0.0178 | 9.6374 | 44.6684 | AID588834 |
| thyroid hormone receptor beta isoform 2 | Rattus norvegicus (Norway rat) | Potency | 21.0756 | 0.0003 | 23.4451 | 159.6830 | AID743065; AID743067 |
| heat shock protein beta-1 | Homo sapiens (human) | Potency | 43.6412 | 0.0420 | 27.3789 | 61.6448 | AID743210; AID743228 |
| mitogen-activated protein kinase 1 | Homo sapiens (human) | Potency | 17.6820 | 0.0398 | 16.7842 | 39.8107 | AID1454; AID995 |
| nuclear factor NF-kappa-B p105 subunit isoform 1 | Homo sapiens (human) | Potency | 44.6684 | 4.4668 | 24.8329 | 44.6684 | AID651749 |
| flap endonuclease 1 | Homo sapiens (human) | Potency | 4.2284 | 0.1337 | 25.4129 | 89.1251 | AID588795 |
| ras-related protein Rab-9A | Homo sapiens (human) | Potency | 73.0780 | 0.0002 | 2.6215 | 31.4954 | AID485297 |
| nuclear factor erythroid 2-related factor 2 isoform 1 | Homo sapiens (human) | Potency | 18.2233 | 0.0006 | 27.2152 | 1,122.0200 | AID651741; AID743202; AID743219 |
| urokinase-type plasminogen activator precursor | Mus musculus (house mouse) | Potency | 12.5893 | 0.1585 | 5.2879 | 12.5893 | AID540303 |
| plasminogen precursor | Mus musculus (house mouse) | Potency | 12.5893 | 0.1585 | 5.2879 | 12.5893 | AID540303 |
| urokinase plasminogen activator surface receptor precursor | Mus musculus (house mouse) | Potency | 12.5893 | 0.1585 | 5.2879 | 12.5893 | AID540303 |
| nuclear receptor ROR-gamma isoform 1 | Mus musculus (house mouse) | Potency | 7.0795 | 0.0079 | 8.2332 | 1,122.0200 | AID2551 |
| geminin | Homo sapiens (human) | Potency | 9.7545 | 0.0046 | 11.3741 | 33.4983 | AID463097; AID624296; AID624297 |
| DNA polymerase kappa isoform 1 | Homo sapiens (human) | Potency | 44.6684 | 0.0316 | 22.3146 | 100.0000 | AID588579 |
| survival motor neuron protein isoform d | Homo sapiens (human) | Potency | 6.3163 | 0.1259 | 12.2344 | 35.4813 | AID1458 |
| cytochrome P450 3A4 isoform 1 | Homo sapiens (human) | Potency | 0.1259 | 0.0316 | 10.2792 | 39.8107 | AID884; AID885 |
| M-phase phosphoprotein 8 | Homo sapiens (human) | Potency | 38.7482 | 0.1778 | 24.7352 | 79.4328 | AID488949 |
| transient receptor potential cation channel subfamily V member 1 | Homo sapiens (human) | Potency | 25.1189 | 0.0912 | 0.0912 | 0.0912 | AID488979 |
| muscarinic acetylcholine receptor M1 | Rattus norvegicus (Norway rat) | Potency | 10.7509 | 0.0010 | 6.0009 | 35.4813 | AID943; AID944 |
| lethal factor (plasmid) | Bacillus anthracis str. A2012 | Potency | 31.6228 | 0.0200 | 10.7869 | 31.6228 | AID912 |
| lamin isoform A-delta10 | Homo sapiens (human) | Potency | 12.5893 | 0.8913 | 12.0676 | 28.1838 | AID1487 |
| neuropeptide S receptor isoform A | Homo sapiens (human) | Potency | 12.5893 | 0.0158 | 12.3113 | 615.5000 | AID1461 |
| Gamma-aminobutyric acid receptor subunit pi | Rattus norvegicus (Norway rat) | Potency | 0.1259 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Polyunsaturated fatty acid lipoxygenase ALOX15B | Homo sapiens (human) | Potency | 6.3096 | 0.3162 | 12.7657 | 31.6228 | AID881 |
| Voltage-dependent calcium channel gamma-2 subunit | Mus musculus (house mouse) | Potency | 27.3060 | 0.0015 | 57.7890 | 15,848.9004 | AID1259244 |
| Interferon beta | Homo sapiens (human) | Potency | 5.3547 | 0.0033 | 9.1582 | 39.8107 | AID1645842 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 5.3547 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| Cellular tumor antigen p53 | Homo sapiens (human) | Potency | 57.4600 | 0.0023 | 19.5956 | 74.0614 | AID651631; AID651743; AID720552 |
| Gamma-aminobutyric acid receptor subunit beta-1 | Rattus norvegicus (Norway rat) | Potency | 0.1259 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit delta | Rattus norvegicus (Norway rat) | Potency | 0.1259 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit gamma-2 | Rattus norvegicus (Norway rat) | Potency | 0.1259 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Glutamate receptor 2 | Rattus norvegicus (Norway rat) | Potency | 27.3060 | 0.0015 | 51.7393 | 15,848.9004 | AID1259244 |
| Gamma-aminobutyric acid receptor subunit alpha-5 | Rattus norvegicus (Norway rat) | Potency | 0.1259 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit alpha-3 | Rattus norvegicus (Norway rat) | Potency | 0.1259 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit gamma-1 | Rattus norvegicus (Norway rat) | Potency | 0.1259 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit alpha-2 | Rattus norvegicus (Norway rat) | Potency | 0.1259 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit alpha-4 | Rattus norvegicus (Norway rat) | Potency | 0.1259 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit gamma-3 | Rattus norvegicus (Norway rat) | Potency | 0.1259 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit alpha-6 | Rattus norvegicus (Norway rat) | Potency | 0.1259 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Alpha-synuclein | Homo sapiens (human) | Potency | 3.4437 | 0.5623 | 9.3985 | 25.1189 | AID652106 |
| Histamine H2 receptor | Cavia porcellus (domestic guinea pig) | Potency | 10.0774 | 0.0063 | 8.2350 | 39.8107 | AID881; AID883 |
| Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | Potency | 24.3595 | 0.0096 | 10.5250 | 35.4813 | AID1479145; AID1479148 |
| Gamma-aminobutyric acid receptor subunit alpha-1 | Rattus norvegicus (Norway rat) | Potency | 0.1259 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit beta-3 | Rattus norvegicus (Norway rat) | Potency | 0.1259 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Guanine nucleotide-binding protein G | Homo sapiens (human) | Potency | 31.6228 | 1.9953 | 25.5327 | 50.1187 | AID624288 |
| Gamma-aminobutyric acid receptor subunit beta-2 | Rattus norvegicus (Norway rat) | Potency | 0.1259 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| TAR DNA-binding protein 43 | Homo sapiens (human) | Potency | 3.5481 | 1.7783 | 16.2081 | 35.4813 | AID652104 |
| GABA theta subunit | Rattus norvegicus (Norway rat) | Potency | 0.1259 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 5.3547 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| ATPase family AAA domain-containing protein 5 | Homo sapiens (human) | Potency | 16.5083 | 0.0119 | 17.9420 | 71.5630 | AID651632; AID720516 |
| Ataxin-2 | Homo sapiens (human) | Potency | 13.9054 | 0.0119 | 12.2221 | 68.7989 | AID588378; AID651632 |
| Gamma-aminobutyric acid receptor subunit epsilon | Rattus norvegicus (Norway rat) | Potency | 0.1259 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 5.3547 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| 25-hydroxyvitamin D-1 alpha hydroxylase, mitochondrial | Homo sapiens (human) | Ki | 0.0725 | 0.0530 | 0.0725 | 0.0920 | AID1799838 |
| Bile salt export pump | Homo sapiens (human) | IC50 (µMol) | 3.4000 | 0.1100 | 7.1903 | 10.0000 | AID1674183 |
| Steroid 17-alpha-hydroxylase/17,20 lyase | Homo sapiens (human) | IC50 (µMol) | 1.1750 | 0.0020 | 0.9818 | 4.7300 | AID1328449; AID1497274; AID1798553 |
| Epoxide hydrolase 1 | Homo sapiens (human) | IC50 (µMol) | 0.0400 | 0.0400 | 2.9800 | 7.0000 | AID1617370 |
| ATP-dependent translocase ABCB1 | Homo sapiens (human) | IC50 (µMol) | 1.0580 | 0.0002 | 2.3185 | 10.0000 | AID1818563 |
| Cytochrome P450 3A4 | Homo sapiens (human) | IC50 (µMol) | 1.1187 | 0.0001 | 1.7536 | 10.0000 | AID1328453; AID1350754; AID1351507; AID1379465; AID1387803; AID1412890; AID1497276; AID1520027; AID1529078; AID1571098; AID1595158; AID1614014; AID1614063; AID1617370; AID1634154; AID1658921; AID1683957; AID1702315; AID1721038; AID1739437; AID1756369; AID1772932; AID1781971; AID1781972; AID1783793; AID1785086; AID1798553; AID1811059; AID1811060; AID1813640; AID1813641; AID1818562; AID1826368; AID1832392; AID1833385; AID1861994; AID1863230; AID1872537; AID1880386; AID1886462; AID1895934; AID1898240; AID1898241; AID1901577; AID1911192 |
| Cytochrome P450 2D6 | Homo sapiens (human) | IC50 (µMol) | 2.7740 | 0.0000 | 2.0151 | 10.0000 | AID1351508; AID1772931; AID1861993 |
| Aromatase | Homo sapiens (human) | IC50 (µMol) | 1.3026 | 0.0000 | 1.2904 | 10.0000 | AID1347596; AID1390539; AID1497275; AID1776977; AID1796255 |
| Cytochrome P450 11B1, mitochondrial | Homo sapiens (human) | IC50 (µMol) | 0.4519 | 0.0005 | 0.2902 | 2.7800 | AID1796205; AID1796255; AID1798553; AID1798554 |
| Cytochrome P450 11B2, mitochondrial | Homo sapiens (human) | IC50 (µMol) | 0.1272 | 0.0001 | 0.2738 | 3.5000 | AID1796205; AID1796255; AID1798554 |
| Cytochrome P450 3A5 | Homo sapiens (human) | IC50 (µMol) | 0.2535 | 0.0033 | 0.7073 | 6.2000 | AID1529074; AID1529075; AID1529076; AID1529077; AID1756369 |
| Bifunctional epoxide hydrolase 2 | Homo sapiens (human) | IC50 (µMol) | 0.0400 | 0.0000 | 0.5450 | 9.1000 | AID1617370 |
| 1,25-dihydroxyvitamin D(3) 24-hydroxylase, mitochondrial | Homo sapiens (human) | IC50 (µMol) | 0.3000 | 0.0023 | 0.3666 | 0.5200 | AID1704644 |
| 1,25-dihydroxyvitamin D(3) 24-hydroxylase, mitochondrial | Homo sapiens (human) | Ki | 0.0280 | 0.0240 | 0.0310 | 0.0350 | AID1799837 |
| Sterol 14-alpha demethylase | Trypanosoma cruzi strain CL Brener | IC50 (µMol) | 0.0140 | 0.0010 | 1.7070 | 10.0000 | AID1882559 |
| Broad substrate specificity ATP-binding cassette transporter ABCG2 | Homo sapiens (human) | IC50 (µMol) | 15.3000 | 0.0040 | 1.9666 | 10.0000 | AID1873201 |
| Estrogen receptor beta | Mus musculus (house mouse) | Ki | 0.0650 | 0.0650 | 0.0777 | 0.0840 | AID221163 |
| Solute carrier family 22 member 1 | Homo sapiens (human) | IC50 (µMol) | 2.6000 | 0.2100 | 5.5537 | 10.0000 | AID1442001 |
| ATP-binding cassette sub-family C member 3 | Homo sapiens (human) | IC50 (µMol) | 133.0000 | 0.6315 | 4.4531 | 9.3000 | AID1473740 |
| Multidrug resistance-associated protein 4 | Homo sapiens (human) | IC50 (µMol) | 69.0000 | 0.2000 | 5.6774 | 10.0000 | AID1473741 |
| 25-hydroxyvitamin D-1 alpha hydroxylase, mitochondrial | Homo sapiens (human) | IC50 (µMol) | 0.3400 | 0.3400 | 0.3400 | 0.3400 | AID1464256 |
| 25-hydroxyvitamin D-1 alpha hydroxylase, mitochondrial | Mus musculus (house mouse) | IC50 (µMol) | 0.3600 | 0.3600 | 0.3600 | 0.3600 | AID1160914; AID1165072 |
| 25-hydroxyvitamin D-1 alpha hydroxylase, mitochondrial | Mus musculus (house mouse) | Ki | 0.0580 | 0.0580 | 0.0580 | 0.0580 | AID1160914; AID1165072 |
| Cytochrome P450 26A1 | Homo sapiens (human) | IC50 (µMol) | 12.0000 | 0.0051 | 3.4125 | 7.8000 | AID282734 |
| Prostaglandin G/H synthase 1 | Bos taurus (cattle) | IC50 (µMol) | 750.0000 | 0.0005 | 1.4128 | 8.2000 | AID160710 |
| Prostaglandin G/H synthase 2 | Bos taurus (cattle) | IC50 (µMol) | 750.0000 | 0.0005 | 0.5739 | 3.4000 | AID160710 |
| Bile salt export pump | Rattus norvegicus (Norway rat) | IC50 (µMol) | 15.6000 | 0.4000 | 2.7500 | 8.6000 | AID1209456 |
| 3',5'-cyclic-AMP phosphodiesterase | Sus scrofa (pig) | IC50 (µMol) | 1,000.0000 | 0.0010 | 3.4002 | 6.4000 | AID158620 |
| Bile salt export pump | Homo sapiens (human) | IC50 (µMol) | 13.7667 | 0.1100 | 7.1903 | 10.0000 | AID1209455; AID1443980; AID1443989; AID1449628; AID1473738; AID681139 |
| Phospholipase A2, major isoenzyme | Sus scrofa (pig) | IC50 (µMol) | 1,000.0000 | 0.0480 | 4.1208 | 8.0000 | AID158620 |
| Chymotrypsinogen A | Bos taurus (cattle) | IC50 (µMol) | 150.0000 | 0.9800 | 4.0560 | 7.2000 | AID52776 |
| Beta-lactamase | Escherichia coli K-12 | IC50 (µMol) | 150.0000 | 0.0150 | 2.4657 | 8.0000 | AID43431 |
| Steroid 17-alpha-hydroxylase/17,20 lyase | Homo sapiens (human) | IC50 (µMol) | 1.5811 | 0.0020 | 0.9818 | 4.7300 | AID1174185; AID1191386; AID1199393; AID1328449; AID207138; AID207139; AID207140; AID207270; AID241487; AID313543; AID315653; AID362147; AID362164; AID362471; AID364749; AID389811; AID426398; AID482322; AID491984; AID499539; AID53211; AID53214; AID53234; AID53236; AID53248; AID53371; AID53373; AID53375; AID53376; AID549785; AID586580; AID592137; AID89274 |
| Steroid 17-alpha-hydroxylase/17,20 lyase | Homo sapiens (human) | Ki | 0.0380 | 0.0380 | 0.3969 | 1.6250 | AID1199393; AID53239 |
| ATP-dependent translocase ABCB1 | Mus musculus (house mouse) | IC50 (µMol) | 6.7000 | 0.0640 | 4.0126 | 10.0000 | AID150754; AID681128 |
| ATP-dependent translocase ABCB1 | Mus musculus (house mouse) | Ki | 6.9300 | 3.5000 | 5.6067 | 6.9300 | AID681138 |
| Aldo-keto reductase family 1 member B1 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 24.2030 | 0.0004 | 1.8773 | 10.0000 | AID625207 |
| Aldo-keto reductase family 1 member B1 | Rattus norvegicus (Norway rat) | Ki | 24.0030 | 0.0032 | 2.2887 | 9.3160 | AID625207 |
| Muscarinic acetylcholine receptor M2 | Homo sapiens (human) | IC50 (µMol) | 26.3460 | 0.0000 | 1.2326 | 7.7930 | AID625152 |
| Muscarinic acetylcholine receptor M2 | Homo sapiens (human) | Ki | 9.3680 | 0.0000 | 0.6902 | 10.0000 | AID625152 |
| ATP-dependent translocase ABCB1 | Homo sapiens (human) | IC50 (µMol) | 12.2540 | 0.0002 | 2.3185 | 10.0000 | AID1176163; AID150618; AID150752; AID150755; AID679463; AID681122; AID681126; AID681127; AID681131; AID681358 |
| ATP-dependent translocase ABCB1 | Homo sapiens (human) | Ki | 10.4567 | 0.0200 | 2.3594 | 8.5900 | AID150735; AID681142; AID681143 |
| Cytochrome P450 3A4 | Homo sapiens (human) | IC50 (µMol) | 1.4592 | 0.0001 | 1.7536 | 10.0000 | AID1066221; AID1152147; AID1164256; AID1168289; AID1176157; AID1195126; AID1229830; AID1244279; AID1252789; AID1254878; AID1281964; AID1301009; AID1310917; AID1328453; AID1450068; AID1472786; AID1495446; AID1557089; AID254813; AID262713; AID311859; AID318316; AID362136; AID362169; AID364764; AID389818; AID394828; AID402936; AID426396; AID428564; AID449589; AID480595; AID491988; AID54780; AID54781; AID54782; AID54783; AID54923; AID566792; AID568746; AID592052; AID625251; AID7232 |
| Cytochrome P450 3A4 | Homo sapiens (human) | Ki | 0.0292 | 0.0001 | 1.4162 | 9.9000 | AID420064; AID437542; AID473745 |
| Steroid 21-hydroxylase | Homo sapiens (human) | IC50 (µMol) | 8.1700 | 0.0007 | 2.3543 | 9.0100 | AID1328451; AID161641 |
| Alpha-2A adrenergic receptor | Homo sapiens (human) | IC50 (µMol) | 19.7830 | 0.0000 | 1.4421 | 7.3470 | AID625201 |
| Alpha-2A adrenergic receptor | Homo sapiens (human) | Ki | 7.4190 | 0.0001 | 0.8074 | 10.0000 | AID625201 |
| Cytochrome P450 2C8 | Homo sapiens (human) | IC50 (µMol) | 0.0600 | 0.0008 | 1.8848 | 7.9000 | AID1254878 |
| Aromatase | Homo sapiens (human) | IC50 (µMol) | 17.5615 | 0.0000 | 1.2904 | 10.0000 | AID1232935; AID1328452; AID262709; AID280107; AID387613; AID436297; AID479369; AID491987; AID53396; AID53566; AID568566; AID654682 |
| Aromatase | Homo sapiens (human) | Ki | 21.9327 | 0.0000 | 0.6046 | 9.5010 | AID53739; AID638445 |
| Steroid 17-alpha-hydroxylase/17,20 lyase | Rattus norvegicus (Norway rat) | IC50 (µMol) | 10.7672 | 0.0016 | 1.6707 | 7.6700 | AID1055880; AID1317746; AID207274; AID207275; AID269148; AID269149; AID270823; AID270825; AID429608; AID429609; AID502080; AID502081; AID53224; AID53228; AID53240; AID53243; AID53378 |
| Polyunsaturated fatty acid 5-lipoxygenase | Rattus norvegicus (Norway rat) | IC50 (µMol) | 25.0000 | 0.0046 | 2.0182 | 10.0000 | AID7062 |
| Polyunsaturated fatty acid lipoxygenase ALOX15 | Oryctolagus cuniculus (rabbit) | IC50 (µMol) | 5.4250 | 0.1100 | 3.2641 | 9.0330 | AID625146 |
| Cholesterol side-chain cleavage enzyme, mitochondrial | Rattus norvegicus (Norway rat) | IC50 (µMol) | 3.3200 | 1.2400 | 3.3200 | 5.4000 | AID53207 |
| 5-hydroxytryptamine receptor 2A | Rattus norvegicus (Norway rat) | IC50 (µMol) | 1.0670 | 0.0004 | 0.9086 | 10.0000 | AID53243 |
| Indoleamine 2,3-dioxygenase 1 | Homo sapiens (human) | IC50 (µMol) | 28.5000 | 0.0537 | 3.0757 | 10.0000 | AID1184068; AID1184069 |
| Cytochrome P450 2A2 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.4560 | 0.3690 | 0.4560 | 0.5430 | AID2916 |
| Cytochrome P450 11B1, mitochondrial | Bos taurus (cattle) | IC50 (µMol) | 0.3800 | 0.0010 | 1.0608 | 7.8300 | AID51046 |
| Cytochrome P450 11B1, mitochondrial | Homo sapiens (human) | IC50 (µMol) | 0.1620 | 0.0005 | 0.2902 | 2.7800 | AID1328450; AID242797; AID255080; AID262707; AID362165; AID491985; AID553065; AID652428 |
| Translocator protein | Rattus norvegicus (Norway rat) | IC50 (µMol) | 3.7600 | 0.0001 | 0.6393 | 4.8100 | AID270823 |
| Alpha-2B adrenergic receptor | Homo sapiens (human) | IC50 (µMol) | 18.0470 | 0.0000 | 1.2380 | 8.1590 | AID625202 |
| Alpha-2B adrenergic receptor | Homo sapiens (human) | Ki | 8.2390 | 0.0002 | 0.7257 | 10.0000 | AID625202 |
| Cytochrome P450 7A1 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 1.2975 | 0.1950 | 1.2975 | 2.4000 | AID51626 |
| Cytochrome P450 11B2, mitochondrial | Homo sapiens (human) | IC50 (µMol) | 0.5179 | 0.0001 | 0.2738 | 3.5000 | AID1177650; AID1177651; AID242795; AID255081; AID262708; AID362166; AID491986; AID553066; AID652429 |
| Estrogen receptor | Mus musculus (house mouse) | Ki | 0.0650 | 0.0650 | 0.0777 | 0.0840 | AID221163 |
| ATP-dependent translocase ABCB1 | Mus musculus (house mouse) | IC50 (µMol) | 3.8000 | 0.2000 | 4.7130 | 10.0000 | AID150753; AID681119 |
| ATP-dependent translocase ABCB1 | Mus musculus (house mouse) | Ki | 12.8000 | 2.1000 | 4.3150 | 7.4800 | AID681137 |
| Substance-K receptor | Homo sapiens (human) | IC50 (µMol) | 17.2430 | 0.0001 | 3.1210 | 9.5530 | AID625227 |
| Substance-K receptor | Homo sapiens (human) | Ki | 5.7480 | 0.0001 | 1.9242 | 9.7930 | AID625227 |
| UDP-glucuronosyltransferase 1A1 | Homo sapiens (human) | IC50 (µMol) | 20.0000 | 0.3000 | 3.2580 | 7.3000 | AID1222388; AID1222389 |
| Sodium-dependent noradrenaline transporter | Homo sapiens (human) | IC50 (µMol) | 24.2030 | 0.0008 | 1.5416 | 20.0000 | AID625207 |
| Sodium-dependent noradrenaline transporter | Homo sapiens (human) | Ki | 24.0030 | 0.0003 | 1.4656 | 10.0000 | AID625207 |
| Thromboxane-A synthase | Homo sapiens (human) | IC50 (µMol) | 2.1650 | 0.0009 | 1.2304 | 10.0000 | AID625229 |
| Histamine H2 receptor | Homo sapiens (human) | IC50 (µMol) | 21.8720 | 0.0220 | 2.2987 | 10.0000 | AID625270 |
| Histamine H2 receptor | Homo sapiens (human) | Ki | 21.5070 | 0.0006 | 2.1973 | 10.0000 | AID625270 |
| Gonadotropin-releasing hormone receptor | Rattus norvegicus (Norway rat) | IC50 (µMol) | 2.0000 | 0.0003 | 0.1542 | 2.0000 | AID102945 |
| Sodium-dependent serotonin transporter | Homo sapiens (human) | IC50 (µMol) | 0.5310 | 0.0001 | 0.8645 | 8.7096 | AID625222 |
| Sodium-dependent serotonin transporter | Homo sapiens (human) | Ki | 0.2820 | 0.0000 | 0.7048 | 8.1930 | AID625222 |
| Type-1 angiotensin II receptor | Oryctolagus cuniculus (rabbit) | IC50 (µMol) | 0.0078 | 0.0001 | 0.0913 | 0.5000 | AID568746 |
| Delta-type opioid receptor | Homo sapiens (human) | IC50 (µMol) | 12.7970 | 0.0002 | 0.7521 | 8.0140 | AID625161 |
| Delta-type opioid receptor | Homo sapiens (human) | Ki | 4.5110 | 0.0000 | 0.5978 | 9.9300 | AID625161 |
| Cytochrome P450 4F2 | Homo sapiens (human) | IC50 (µMol) | 1.6000 | 1.6000 | 4.2667 | 6.2000 | AID1216149 |
| Sodium-dependent dopamine transporter | Homo sapiens (human) | IC50 (µMol) | 23.5170 | 0.0007 | 1.8419 | 46.0000 | AID625256 |
| Sodium-dependent dopamine transporter | Homo sapiens (human) | Ki | 18.6850 | 0.0002 | 1.1115 | 8.0280 | AID625256 |
| 1,25-dihydroxyvitamin D(3) 24-hydroxylase, mitochondrial | Homo sapiens (human) | IC50 (µMol) | 0.4144 | 0.0023 | 0.3666 | 0.5200 | AID1160913; AID1165071; AID1464255; AID1486357; AID282480; AID492340; AID492341; AID492342; AID514964 |
| 1,25-dihydroxyvitamin D(3) 24-hydroxylase, mitochondrial | Homo sapiens (human) | Ki | 0.0340 | 0.0240 | 0.0310 | 0.0350 | AID1160913; AID1165071 |
| Potassium voltage-gated channel subfamily H member 2 | Homo sapiens (human) | IC50 (µMol) | 1.9036 | 0.0009 | 1.9014 | 10.0000 | AID161281; AID243151; AID397743; AID408340; AID576612 |
| Sodium/bile acid cotransporter | Homo sapiens (human) | IC50 (µMol) | 264.0000 | 1.0000 | 5.9267 | 9.6000 | AID681378 |
| Lanosterol 14-alpha demethylase | Homo sapiens (human) | IC50 (µMol) | 0.1900 | 0.0500 | 1.4390 | 4.0000 | AID322753 |
| Lanosterol 14-alpha demethylase | Homo sapiens (human) | Ki | 0.0440 | 0.0245 | 0.0440 | 0.0635 | AID221159; AID221160 |
| Cytochrome P450 7A1 | Mus musculus (house mouse) | IC50 (µMol) | 1.2975 | 0.1950 | 1.2975 | 2.4000 | AID51626 |
| Lanosterol 14-alpha demethylase | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0830 | 0.0470 | 0.0830 | 0.1190 | AID54929 |
| Lanosterol 14-alpha demethylase | Rattus norvegicus (Norway rat) | Ki | 0.0650 | 0.0057 | 0.0353 | 0.0650 | AID221163 |
| Canalicular multispecific organic anion transporter 1 | Homo sapiens (human) | IC50 (µMol) | 133.0000 | 2.4100 | 6.3433 | 10.0000 | AID1473739 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Cytochrome P450 3A4 | Homo sapiens (human) | Kd | 0.9000 | 0.0130 | 0.4565 | 0.9000 | AID1529094 |
| Cytochrome P450 3A5 | Homo sapiens (human) | Kd | 3.1000 | 0.1000 | 1.6000 | 3.1000 | AID1529090 |
| Cytochrome P450 144 | Mycobacterium tuberculosis CDC1551 | Kd | 60.7000 | 0.3600 | 2.5990 | 5.3000 | AID1799791 |
| Steroid C26-monooxygenase | Mycobacterium tuberculosis CDC1551 | Kd | 60.7000 | 0.1000 | 2.5967 | 6.1000 | AID1799791 |
| Steroid C26-monooxygenase | Mycobacterium tuberculosis CDC1551 | Kd | 60.7000 | 0.3600 | 2.5990 | 5.3000 | AID1799791 |
| Sterol 14-alpha demethylase | Trypanosoma cruzi strain CL Brener | Kd | 1.1600 | 0.0180 | 0.4285 | 2.3000 | AID1799528 |
| Gonadotropin-releasing hormone receptor | Rattus norvegicus (Norway rat) | Kd | 0.2705 | 0.0002 | 0.2705 | 0.8110 | AID100101; AID100102; AID102949 |
| Lanosterol 14-alpha demethylase | Homo sapiens (human) | Kd | 2.7400 | 0.1100 | 2.7400 | 8.0000 | AID322375; AID322755; AID572704 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| heat shock protein HSP 90-alpha isoform 2 | Homo sapiens (human) | AC50 | 0.4350 | 0.1950 | 3.6679 | 18.6960 | AID540270 |
| heat shock protein 90, putative | Plasmodium falciparum 3D7 | AC50 | 1.2860 | 0.1950 | 4.9920 | 98.5000 | AID540268 |
| Camphor 5-monooxygenase | Pseudomonas putida | Ks | 0.5500 | 0.5000 | 0.5500 | 0.6000 | AID54948; AID99365 |
| Epoxide hydrolase 1 | Rattus norvegicus (Norway rat) | E100 | 54.0000 | 6.2000 | 6.2000 | 6.2000 | AID208343 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1159607 | Screen for inhibitors of RMI FANCM (MM2) intereaction | 2016 | Journal of biomolecular screening, Jul, Volume: 21, Issue:6 | A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway. |
| AID1578467 | Drug concentration in total skeletal muscle in Wistar Han rat at 1 to 2 mg/kg, iv infused for 10 to 20 hrs by LC-MS/MS analysis | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Structural attributes influencing unbound tissue distribution. |
| AID1811060 | Inhibition of human CYP3A4 using midazolam as substrate in presence of NADPH incubated for 15 to 45 mins | 2021 | Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14 | Improving Druggability of Novel Diarylpyrimidine NNRTIs by a Fragment-Based Replacement Strategy: From Biphenyl-DAPYs to Heteroaromatic-Biphenyl-DAPYs. |
| AID1399508 | Fungicidal activity against Aspergillus fumigatus isolate 1022 after 144 hrs by serial dilution assay | 2018 | Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16 | 5-Adamantan thiadiazole-based thiazolidinones as antimicrobial agents. Design, synthesis, molecular docking and evaluation. |
| AID1412941 | Antifungal activity against Penicillium ochrochloron ATCC 9112 by microdilution method | 2018 | MedChemComm, May-01, Volume: 9, Issue:5 | Design, synthesis and antimicrobial activity of usnic acid derivatives. |
| AID1596690 | Antifungal activity against Aspergillus niger ATCC 6275 after 72 hrs by microdilution technique | 2019 | European journal of medicinal chemistry, Aug-01, Volume: 175 | Appendix A. dithioloquinolinethiones as new potential multitargeted antibacterial and antifungal agents: Synthesis, biological evaluation and molecular docking studies. |
| AID1369444 | Antifungal activity against Candida albicans SP3931 after 48 hrs by broth microdilution method | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9 | Combating Drug-Resistant Fungi with Novel Imperfectly Amphipathic Palindromic Peptides. |
| AID1898241 | Inhibition of CYP3A4 in human liver microsomes using testosterone as substrate in presence of NADPH | |||
| AID1634154 | Inhibition of CYP3A4 (unknown origin) | 2019 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16 | Strategies for the development of highly selective cytochrome P450 inhibitors: Several CYP targets in current research. |
| AID1578465 | Drug concentration in total heart in Wistar Han rat at 1 to 2 mg/kg, iv infused for 10 to 20 hrs by LC-MS/MS analysis | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Structural attributes influencing unbound tissue distribution. |
| AID1574941 | Inhibition of CYP2C9 in human liver microsomes assessed as residual activity at 10 uM using tolbutamide as substrate preincubated for 5 mins followed by NADPH addition and measured after 15 mins by LC-MS/MS analysis relative to control | 2019 | Bioorganic & medicinal chemistry letters, 02-01, Volume: 29, Issue:3 | Click chemistry for improvement in selectivity of quinazoline-based kinase inhibitors for mutant epidermal growth factor receptors. |
| AID1399511 | Antifungal activity against Aspergillus ochraceus ATCC 12066 after 72 hrs by serial dilution assay | 2018 | Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16 | 5-Adamantan thiadiazole-based thiazolidinones as antimicrobial agents. Design, synthesis, molecular docking and evaluation. |
| AID1721988 | Antifungal activity Penicillium verrucosum var. cyclopium by microdilution method | 2020 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 30, Issue:17 | New vinyl-1,2,4-triazole derivatives as antimicrobial agents: Synthesis, biological evaluation and molecular docking studies. |
| AID1572083 | Inhibition of CYP3A4 in human liver microsomes using midazolam as substrate after 10 mins in presence of NADPH | 2019 | Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3 | Identification of Dihydrofuro[3,4- d]pyrimidine Derivatives as Novel HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors with Promising Antiviral Activities and Desirable Physicochemical Properties. |
| AID1703908 | Permeability of the compound by PAMPA-TGI assay | 2020 | European journal of medicinal chemistry, Oct-15, Volume: 204 | Discovery of sulfonyl hydrazone derivative as a new selective PDE4A and PDE4D inhibitor by lead-optimization approach on the prototype LASSBio-448: In vitro and in vivo preclinical studies. |
| AID1402884 | Antifungal activity against Candida parapsilosis ATCC 22019 by broth microdilution assay | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | The synthesis, antifungal and apoptotic effects of triazole-oxadiazoles against Candida species. |
| AID1369453 | Antifungal activity against Candida tropicalis cgmcc 2.1975 after 48 hrs by broth microdilution method | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9 | Combating Drug-Resistant Fungi with Novel Imperfectly Amphipathic Palindromic Peptides. |
| AID1596696 | Antifungal activity against Penicillium funiculosum ATCC 36839 after 72 hrs by microdilution technique | 2019 | European journal of medicinal chemistry, Aug-01, Volume: 175 | Appendix A. dithioloquinolinethiones as new potential multitargeted antibacterial and antifungal agents: Synthesis, biological evaluation and molecular docking studies. |
| AID1578462 | Total plasma concentration in Wistar Han rat at 1 to 2 mg/kg, iv infused for 10 to 20 hrs by LC-MS/MS analysis | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Structural attributes influencing unbound tissue distribution. |
| AID1918335 | Antifungal activity against Candida tropicalis ATCC 1369 assessed as inhibition of fungal growth measured after 72 hrs by CLSI based liquid medium dilution method | 2022 | Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21 | Novel Aryl Alkamidazole Derivatives as Multifunctional Antifungal Inhibitors: Design, Synthesis, and Biological Evaluation. |
| AID1604176 | Antileishmanial activity against Leishmania amazonensis MHOM/BR/77/LTB 0016 promastigotes assessed as reduction in parasite viability after 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Multi-target drugs active against leishmaniasis: A paradigm of drug repurposing. |
| AID1403676 | Antifungal activity against Aspergillus niger assessed as diameter of inhibition zone at 25 ug/well after 48 hrs by agar well diffusion method | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Synthesis and antimicrobial activity of pyrimidinyl 1,3,4-oxadiazoles, 1,3,4-thiadiazoles and 1,2,4-triazoles. |
| AID1662935 | Antifungal activity against Geotrichum candidum assessed as fungal growth inhibition by micro-dilution method | 2020 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 30, Issue:13 | Design, synthesis and evaluation of hydrazine and acyl hydrazone derivatives of 5-pyrrolidin-2-one as antifungal agents. |
| AID1412935 | Antifungal activity against Aspergillus fumigatus ATCC 1022 by microdilution method | 2018 | MedChemComm, May-01, Volume: 9, Issue:5 | Design, synthesis and antimicrobial activity of usnic acid derivatives. |
| AID1537285 | Antifungal activity against Cercospora personata after 3 to 7 days by microbroth dilution method | 2019 | Journal of natural products, 02-22, Volume: 82, Issue:2 | Prenylated Indole Diterpene Alkaloids from a Mine-Soil-Derived Tolypocladium sp. |
| AID1546114 | Antifungal activity against Candida albicans | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | Current scenario of tetrazole hybrids for antibacterial activity. |
| AID1399523 | Antifungal activity against Penicillium cyclopium var verucosum after 72 hrs by serial dilution assay | 2018 | Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16 | 5-Adamantan thiadiazole-based thiazolidinones as antimicrobial agents. Design, synthesis, molecular docking and evaluation. |
| AID1713217 | Antiproliferative activity against androgen-sensitive human LNCAP cells assessed as inhibition of testosterone-induced cell growth at 50 uM incubated for 48 hrs by sulforhodamine B assay relative to control | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Synthesis of 17β-N-arylcarbamoylandrost-4-en-3-one derivatives and their anti-proliferative effect on human androgen-sensitive LNCaP cell line. |
| AID1713220 | Growth inhibition of androgen-sensitive human LNCAP cells incubated for 48 hrs by sulforhodamine B assay | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Synthesis of 17β-N-arylcarbamoylandrost-4-en-3-one derivatives and their anti-proliferative effect on human androgen-sensitive LNCaP cell line. |
| AID1572372 | Inhibition of human CYP3A4 in human liver microsomes at 50 times IC50 concentration relative to control | 2019 | Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3 | Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 Inhibitors. |
| AID1578463 | Drug concentration in total white adipose tissue in Wistar Han rat at 1 to 2 mg/kg, iv infused for 10 to 20 hrs by LC-MS/MS analysis | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Structural attributes influencing unbound tissue distribution. |
| AID1596694 | Antifungal activity against Penicillium ochrochloron ATCC 9112 after 72 hrs by microdilution technique | 2019 | European journal of medicinal chemistry, Aug-01, Volume: 175 | Appendix A. dithioloquinolinethiones as new potential multitargeted antibacterial and antifungal agents: Synthesis, biological evaluation and molecular docking studies. |
| AID1484689 | Antileishmanial activity against Leishmania major MHOM/SN/74/Seidman promastigote forms after 8 days | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | An overview of azoles targeting sterol 14α-demethylase for antileishmanial therapy. |
| AID1411635 | Antifungal activity against Aspergillus fumigatus after 72 hrs by serial dilution method | |||
| AID1864876 | Antifungal activity against Cryptococcus neoformans ZKCC 2209 assessed as fungal growth inhibition measured after 72 hrs by double dilution method | |||
| AID1595121 | Antifungal activity against Candida albicans NCCS 3471 assessed as inhibition zone at 10 ug/ml incubated for 3 to 4 days by disk diffusion method | 2019 | European journal of medicinal chemistry, May-15, Volume: 170 | Tetrazole hybrids and their antifungal activities. |
| AID1918332 | Antifungal activity against Candida albicans ATCC SC5314 assessed as inhibition of fungal growth measured after 72 hrs by CLSI based liquid medium dilution method | 2022 | Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21 | Novel Aryl Alkamidazole Derivatives as Multifunctional Antifungal Inhibitors: Design, Synthesis, and Biological Evaluation. |
| AID1596686 | Antifungal activity against Aspergillus versicolor ATCC 11730 after 72 hrs by microdilution method | 2019 | European journal of medicinal chemistry, Aug-01, Volume: 175 | Appendix A. dithioloquinolinethiones as new potential multitargeted antibacterial and antifungal agents: Synthesis, biological evaluation and molecular docking studies. |
| AID1918334 | Antifungal activity against Candida krusei ATCC 6258 assessed as inhibition of fungal growth measured after 72 hrs by CLSI based liquid medium dilution method | 2022 | Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21 | Novel Aryl Alkamidazole Derivatives as Multifunctional Antifungal Inhibitors: Design, Synthesis, and Biological Evaluation. |
| AID1402881 | Antifungal activity against Candida albicans ATCC 90028 by broth microdilution assay | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | The synthesis, antifungal and apoptotic effects of triazole-oxadiazoles against Candida species. |
| AID1678800 | Antimalarial activity against chloroquine sensitive Plasmodium falciparum | 2020 | RSC medicinal chemistry, Feb-01, Volume: 11, Issue:2 | An epigrammatic status of the ' |
| AID1596691 | Fungicidal activity against Aspergillus niger ATCC 6275 incubated for 72 hrs followed by sub-culturing on broth malt medium and measured after 72 hrs | 2019 | European journal of medicinal chemistry, Aug-01, Volume: 175 | Appendix A. dithioloquinolinethiones as new potential multitargeted antibacterial and antifungal agents: Synthesis, biological evaluation and molecular docking studies. |
| AID1412948 | Antifungal activity against Penicillium verrucosum var. cyclopium food isolate by microdilution method | 2018 | MedChemComm, May-01, Volume: 9, Issue:5 | Design, synthesis and antimicrobial activity of usnic acid derivatives. |
| AID1861994 | Inhibition of CYP3A4 (unknown origin) using BOMCC as a substrate | 2022 | Bioorganic & medicinal chemistry, 09-01, Volume: 69 | Design, synthesis, and biological evaluation of a new series of pyrazole derivatives: Discovery of potent and selective JNK3 kinase inhibitors. |
| AID1864881 | Antifungal activity against Aspergillus fumigatus KM8001 assessed as fungal growth inhibition measured after 72 hrs by double dilution method | |||
| AID1713216 | Antiproliferative activity against androgen-sensitive human LNCAP cells assessed as inhibition of cell growth at 50 uM incubated for 48 hrs by sulforhodamine B assay relative to control | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Synthesis of 17β-N-arylcarbamoylandrost-4-en-3-one derivatives and their anti-proliferative effect on human androgen-sensitive LNCaP cell line. |
| AID1392840 | Inhibition of CYP3A4 in human liver microsomes using midazolam as substrate preincubated for 10 mins followed by NADPH addition measured after 10 mins by LC-MS/MS analysis | 2018 | Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12 | Design, synthesis and evaluation of benzoheterocycle analogues as potent antifungal agents targeting CYP51. |
| AID1399513 | Antifungal activity against Aspergillus niger ATCC 6275 after 72 hrs by serial dilution assay | 2018 | Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16 | 5-Adamantan thiadiazole-based thiazolidinones as antimicrobial agents. Design, synthesis, molecular docking and evaluation. |
| AID1595080 | Antifungal activity against Candida tropicalis by broth microdilution method | 2019 | European journal of medicinal chemistry, May-15, Volume: 170 | Tetrazole hybrids and their antifungal activities. |
| AID1388201 | Antifungal activity against Trichoderma reesei ATCC 13631 at 100 ug/ml incubated for 72 hrs by agar disc diffusion assay | 2017 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 27, Issue:18 | Synthesis, antimicrobial activity, structure-activity relationship and cytotoxic studies of a new series of functionalized (Z)-3-(2-oxo-2-substituted ethylidene)-3,4-dihydro-2H-benzo[b][1,4]oxazin-2-ones. |
| AID1529080 | Cytotoxicity against wild type human AsPC1 cells assessed as cell growth | 2020 | Journal of medicinal chemistry, 02-13, Volume: 63, Issue:3 | Clobetasol Propionate Is a Heme-Mediated Selective Inhibitor of Human Cytochrome P450 3A5. |
| AID1604267 | Inhibition of rat spleen microsome HO-1 preincubated for 10 mins followed by beta-NADPH addition and measured after 15 mins by gas chromatography | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Heme Oxygenase-2 (HO-2) as a therapeutic target: Activators and inhibitors. |
| AID1571098 | Inhibition of CYP3A4 (unknown origin) using beetle D-luciferin as substrate by CYP450-Glo assay | 2018 | MedChemComm, Nov-01, Volume: 9, Issue:11 | Search for a 5-CT alternative. |
| AID1595122 | Antifungal activity against Aspergillus fumigatus NCIM 902 assessed as inhibition zone at 10 ug/ml incubated for 3 to 4 days by disk diffusion method | 2019 | European journal of medicinal chemistry, May-15, Volume: 170 | Tetrazole hybrids and their antifungal activities. |
| AID1399509 | Antifungal activity against Aspergillus versicolor ATCC 11730 after 72 hrs by serial dilution assay | 2018 | Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16 | 5-Adamantan thiadiazole-based thiazolidinones as antimicrobial agents. Design, synthesis, molecular docking and evaluation. |
| AID1565030 | Kinetic aqueous solubility of the compound in pH 7.46 phosphate buffer at 100 uM incubated for 120 mins by LC-MS/MS analysis | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Discovery of aryl-substituted indole and indoline derivatives as RORγt agonists. |
| AID1365723 | Solubility of compound in Middlebrook 7H9 broth media at pH 6.4 at 200 uM after 90 mins by UV-VIS spectrophotometric method | 2017 | Bioorganic & medicinal chemistry, 11-01, Volume: 25, Issue:21 | The antitubercular activity of various nitro(triazole/imidazole)-based compounds. |
| AID1411644 | Antifungal activity against Penicillium funiculosum ATCC 36839 after 72 hrs by serial dilution method | |||
| AID1703889 | Permeability of the compound incubated for 8 hrs by PAMPA-TGI assay | 2020 | European journal of medicinal chemistry, Oct-15, Volume: 204 | Discovery of sulfonyl hydrazone derivative as a new selective PDE4A and PDE4D inhibitor by lead-optimization approach on the prototype LASSBio-448: In vitro and in vivo preclinical studies. |
| AID1529076 | Inhibition of CYP3A5 in doxycycline-induced CYP3A5 overexpressing wild type human AsPC1 cells assessed as decrease in 1-hydroxymidazolam formation using midazolam as substrate pretreated with doxycycline for 24 hrs followed by incubation with compound for | 2020 | Journal of medicinal chemistry, 02-13, Volume: 63, Issue:3 | Clobetasol Propionate Is a Heme-Mediated Selective Inhibitor of Human Cytochrome P450 3A5. |
| AID1627896 | Antifungal activity against Candida albicans MTCC 227 after 48 to 72 hrs at 28 degC by two fold serial dilution method | 2016 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 26, Issue:17 | Gold catalyzed double condensation reaction: Synthesis, antimicrobial and cytotoxicity of spirooxindole derivatives. |
| AID1729768 | Fungicidal activity against Candida albicans isolate 3 assessed as fungal killing incubated for 48 hrs followed by plating on SD agar plate | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Design, synthesis, and biodistribution studies of new analogues of marine alkaloids: Potent in vitro and in vivo fungicidal agents against Candida spp. |
| AID1403679 | Antifungal activity against Penicillium chrysogenum assessed as diameter of inhibition zone at 12.5 ug/well after 48 hrs by agar well diffusion method | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Synthesis and antimicrobial activity of pyrimidinyl 1,3,4-oxadiazoles, 1,3,4-thiadiazoles and 1,2,4-triazoles. |
| AID1390539 | Inhibition of aromatase in supersomes (unknown origin) using 7-methoxy-4-trifloromethyl coumarone as substrate after 30 mins by fluorescence assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Studies on non-steroidal inhibitors of aromatase enzyme; 4-(aryl/heteroaryl)-2-(pyrimidin-2-yl)thiazole derivatives. |
| AID1683957 | Inhibition of CYP3A4 in in human liver microsomes at incubated for 10 mins in presence of CYP3A4 substrate/NADP+ by fluorescence based assay | |||
| AID1578461 | Fraction unbound in Wistar Han rat skeletal muscle at 2 uM incubated for 6 hrs by equilibrium dialysis method | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Structural attributes influencing unbound tissue distribution. |
| AID1772931 | Inhibition of CYP2D6 (unknown origin) using EOMCC as a substrate incubated for 20 mins by fluorescence based analysis | 2021 | European journal of medicinal chemistry, Nov-15, Volume: 224 | Discovery of first-in-class imidazothiazole-based potent and selective ErbB4 (HER4) kinase inhibitors. |
| AID1369443 | Antifungal activity against Candida albicans cgmcc 2.2086 after 48 hrs by broth microdilution method | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9 | Combating Drug-Resistant Fungi with Novel Imperfectly Amphipathic Palindromic Peptides. |
| AID1785086 | Inhibition of human recombinant CYP3A4 by fluorescence assay | |||
| AID1729769 | Fungicidal activity against Candida albicans isolate 4 assessed as fungal killing incubated for 48 hrs followed by plating on SD agar plate | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Design, synthesis, and biodistribution studies of new analogues of marine alkaloids: Potent in vitro and in vivo fungicidal agents against Candida spp. |
| AID1412936 | Antifungal activity against Aspergillus versicolor ATCC 11730 by microdilution method | 2018 | MedChemComm, May-01, Volume: 9, Issue:5 | Design, synthesis and antimicrobial activity of usnic acid derivatives. |
| AID1596693 | Fungicidal activity against Trichoderma viride IAM 5061 incubated for 72 hrs followed by sub-culturing on broth malt medium and measured after 72 hrs | 2019 | European journal of medicinal chemistry, Aug-01, Volume: 175 | Appendix A. dithioloquinolinethiones as new potential multitargeted antibacterial and antifungal agents: Synthesis, biological evaluation and molecular docking studies. |
| AID1721985 | Antifungal activity Trichoderma viride by microdilution method | 2020 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 30, Issue:17 | New vinyl-1,2,4-triazole derivatives as antimicrobial agents: Synthesis, biological evaluation and molecular docking studies. |
| AID1529065 | Inhibition of human recombinant CYP3A4 expressed in supersomes assessed as decrease in formation of D-luciferin at 1.89 uM using luciferin-IPA as substrate incubated for 10 mins in presence of NADPH by P450-Glo luminescence assay relative to control | 2020 | Journal of medicinal chemistry, 02-13, Volume: 63, Issue:3 | Clobetasol Propionate Is a Heme-Mediated Selective Inhibitor of Human Cytochrome P450 3A5. |
| AID1572536 | Inhibition of CYP3A4 in human liver microsomes using testosterone as substrate after 10 mins in presence of NADP by LC-MS/MS analysis | |||
| AID1411648 | Fungicidal activity against Candida albicans incubated for 72 hrs followed by serial sub-cultivation for 72 hrs and measured after 72 hrs by serial dilution method | |||
| AID1729762 | Fungicidal activity against Candida albicans ATCC 10231 assessed as fungal killing incubated for 48 hrs followed by plating on SD agar plate | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Design, synthesis, and biodistribution studies of new analogues of marine alkaloids: Potent in vitro and in vivo fungicidal agents against Candida spp. |
| AID1578459 | Fraction unbound in Wistar Han rat heart at 2 uM incubated for 6 hrs by equilibrium dialysis method | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Structural attributes influencing unbound tissue distribution. |
| AID1546123 | Antifungal activity against Aspergillus niger assessed as zone of inhibition at 250 ug/ml | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | Current scenario of tetrazole hybrids for antibacterial activity. |
| AID1399507 | Antifungal activity against Aspergillus fumigatus isolate 1022 after 72 hrs by serial dilution assay | 2018 | Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16 | 5-Adamantan thiadiazole-based thiazolidinones as antimicrobial agents. Design, synthesis, molecular docking and evaluation. |
| AID1729766 | Fungicidal activity against Candida albicans isolate 1 assessed as fungal killing incubated for 48 hrs followed by plating on SD agar plate | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Design, synthesis, and biodistribution studies of new analogues of marine alkaloids: Potent in vitro and in vivo fungicidal agents against Candida spp. |
| AID1721991 | Fungicidal activity Aspergillus ochraceus | 2020 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 30, Issue:17 | New vinyl-1,2,4-triazole derivatives as antimicrobial agents: Synthesis, biological evaluation and molecular docking studies. |
| AID1369446 | Antifungal activity against Candida albicans SP3902 after 48 hrs by broth microdilution method | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9 | Combating Drug-Resistant Fungi with Novel Imperfectly Amphipathic Palindromic Peptides. |
| AID1713218 | Antiproliferative activity against androgen-sensitive human LNCAP cells assessed as inhibition of DHT-induced cell growth at 50 uM incubated for 48 hrs by sulforhodamine B assay relative to control | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Synthesis of 17β-N-arylcarbamoylandrost-4-en-3-one derivatives and their anti-proliferative effect on human androgen-sensitive LNCaP cell line. |
| AID1412942 | Fungicidal activity against Penicillium funiculosum ATCC 36839 by microdilution method | 2018 | MedChemComm, May-01, Volume: 9, Issue:5 | Design, synthesis and antimicrobial activity of usnic acid derivatives. |
| AID1571579 | Antimicrobial activity against Trichophyton mentagrophytes var. gypseum 1773 measured after 14 days by two-fold serial dilution method | 2018 | MedChemComm, Dec-01, Volume: 9, Issue:12 | Design, synthesis, and biological activity of novel ammonium salts containing sterically hindered phenolic fragment and phosphoryl group. |
| AID1412940 | Antifungal activity against Penicillium funiculosum ATCC 36839 by microdilution method | 2018 | MedChemComm, May-01, Volume: 9, Issue:5 | Design, synthesis and antimicrobial activity of usnic acid derivatives. |
| AID1561313 | Inhibition of CYP3A in rat liver microsomes assessed as reduction in aminopyrine N-demethylase activity preincubated for 3 mins followed by NADPH addition and measured after 15 mins by iodometric titration method | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Discovery of Highly Potent Benzimidazole Derivatives as Indoleamine 2,3-Dioxygenase-1 (IDO1) Inhibitors: From Structure-Based Virtual Screening to |
| AID1721993 | Fungicidal activity Trichoderma viride | 2020 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 30, Issue:17 | New vinyl-1,2,4-triazole derivatives as antimicrobial agents: Synthesis, biological evaluation and molecular docking studies. |
| AID1729775 | Fungicidal activity against Candida albicans isolate 10 assessed as fungal killing incubated for 48 hrs followed by plating on SD agar plate | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Design, synthesis, and biodistribution studies of new analogues of marine alkaloids: Potent in vitro and in vivo fungicidal agents against Candida spp. |
| AID1402900 | Induction of apoptosis in Candida parapsilosis ATCC 22019 assessed as late apoptotic cells at antifungal MIC90 after 24 hrs by Annexin V/propidium iodide staining based flow cytometry (Rvb = 0.9%) | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | The synthesis, antifungal and apoptotic effects of triazole-oxadiazoles against Candida species. |
| AID1369459 | Fungicidal activity against Candida albicans SP3902 after 96 hrs | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9 | Combating Drug-Resistant Fungi with Novel Imperfectly Amphipathic Palindromic Peptides. |
| AID1595079 | Antifungal activity against Candida glabrata ATCC 36583 by broth microdilution method | 2019 | European journal of medicinal chemistry, May-15, Volume: 170 | Tetrazole hybrids and their antifungal activities. |
| AID1497275 | Inhibition of CYP19 (unknown origin) by Becton Dickinson aromatase assay | 2018 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 28, Issue:13 | Design and synthesis of functionalized piperazin-1yl-(E)-stilbenes as inhibitors of 17α-hydroxylase-C17,20-lyase (Cyp17). |
| AID1369461 | Fungicidal activity against Candida albicans isolated from alveolar fluid after 96 hrs | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9 | Combating Drug-Resistant Fungi with Novel Imperfectly Amphipathic Palindromic Peptides. |
| AID1484707 | Antileishmanial activity against Leishmania amazonensis LV78 axenic amastigote forms after 8 days | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | An overview of azoles targeting sterol 14α-demethylase for antileishmanial therapy. |
| AID1634153 | Antifungal activity against Candida albicans | 2019 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16 | Strategies for the development of highly selective cytochrome P450 inhibitors: Several CYP targets in current research. |
| AID1627886 | Antifungal activity against Malassezia pachydermatis at 1 mg/disc after 48 hrs at 28 degC by disc diffusion method | 2016 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 26, Issue:17 | Gold catalyzed double condensation reaction: Synthesis, antimicrobial and cytotoxicity of spirooxindole derivatives. |
| AID1402889 | Induction of apoptosis in Candida albicans ATCC 90028 assessed as necrotic cells at antifungal MIC90 after 24 hrs by Annexin V/propidium iodide staining based flow cytometry (Rvb = 0.2%) | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | The synthesis, antifungal and apoptotic effects of triazole-oxadiazoles against Candida species. |
| AID1818563 | Inhibition of wild type human P-gp in human MES-SA/Dx5 cells incubated for 3 days by MTT assay | 2022 | Journal of medicinal chemistry, 01-13, Volume: 65, Issue:1 | Discovery and Characterization of Potent Dual P-Glycoprotein and CYP3A4 Inhibitors: Design, Synthesis, Cryo-EM Analysis, and Biological Evaluations. |
| AID1729774 | Fungicidal activity against Candida albicans isolate 9 assessed as fungal killing incubated for 48 hrs followed by plating on SD agar plate | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Design, synthesis, and biodistribution studies of new analogues of marine alkaloids: Potent in vitro and in vivo fungicidal agents against Candida spp. |
| AID1872537 | Inhibition of CYP3A4 in human hepatocyte microsomes using testosterone as substrate by LC-MS/MS analysis | 2022 | European journal of medicinal chemistry, Mar-05, Volume: 231 | Synthetic approaches and structural diversity of triazolylbutanols derived from voriconazole in the antifungal drug development. |
| AID1411636 | Fungicidal activity against Aspergillus fumigatus incubated for 72 hrs followed by serial sub-cultivation for 72 hrs and measured after 72 hrs by serial dilution method | |||
| AID1891105 | Plasma protein binding in Sprague-Dawley rat plasma at 10 uM incubated for 6 hrs by LC-MS/MS based equilibrium dialysis method | 2022 | European journal of medicinal chemistry, Jun-05, Volume: 236 | Synthesis and biological evaluation of 1,2,4-triazole derivatives as potential Nrf2 activators for the treatment of cerebral ischemic injury. |
| AID1595075 | Antifungal activity against Candida albicans | 2019 | European journal of medicinal chemistry, May-15, Volume: 170 | Tetrazole hybrids and their antifungal activities. |
| AID1596695 | Fungicidal activity against Penicillium ochrochloron ATCC 9112 incubated for 72 hrs followed by sub-culturing on broth malt medium and measured after 72 hrs | 2019 | European journal of medicinal chemistry, Aug-01, Volume: 175 | Appendix A. dithioloquinolinethiones as new potential multitargeted antibacterial and antifungal agents: Synthesis, biological evaluation and molecular docking studies. |
| AID1918341 | Antifungal activity against fluconazole-resistant Candida albicans 904 assessed as inhibition of fungal growth measured after 72 hrs by CLSI based liquid medium dilution method | 2022 | Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21 | Novel Aryl Alkamidazole Derivatives as Multifunctional Antifungal Inhibitors: Design, Synthesis, and Biological Evaluation. |
| AID1604177 | Antileishmanial activity against Leishmania amazonensis MHOM/BR/77/LTB 0016 intracellular amastigotes infected in BALB/c Peritoneal macrophages assessed as reduction in parasite viability after 72 hrs by light microscopic method | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Multi-target drugs active against leishmaniasis: A paradigm of drug repurposing. |
| AID1729761 | Fungicidal activity against Candida albicans ATCC 18804 assessed as fungal killing incubated for 48 hrs followed by plating on SD agar plate | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Design, synthesis, and biodistribution studies of new analogues of marine alkaloids: Potent in vitro and in vivo fungicidal agents against Candida spp. |
| AID1656769 | Induction of human HMGCR-dCat-ELuc degradation expressed in HEK293 cells assessed as reduction in luciferase activity measured after 8 hrs by luciferase reporter assay | 2020 | Bioorganic & medicinal chemistry, 02-01, Volume: 28, Issue:3 | Luciferase-based HMG-CoA reductase degradation assay for activity and selectivity profiling of oxy(lano)sterols. |
| AID1369478 | Antifungal activity against Candida albicans cgmcc 2.2086 in presence of KCl by broth dilution method | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9 | Combating Drug-Resistant Fungi with Novel Imperfectly Amphipathic Palindromic Peptides. |
| AID1546155 | Antimicrobial activity against Escherichia coli assessed as zone of inhibition at 10 ug/ml | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | Current scenario of tetrazole hybrids for antibacterial activity. |
| AID1729756 | Antifungal activity against Candida albicans isolate 9 assessed as reduction in fungal growth incubated for 48 hrs by broth microdilution method | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Design, synthesis, and biodistribution studies of new analogues of marine alkaloids: Potent in vitro and in vivo fungicidal agents against Candida spp. |
| AID1872788 | Antifungal activity against Fusarium solani assessed as zone of inhibition | 2022 | European journal of medicinal chemistry, Apr-15, Volume: 234 | Recent applications of vinyl sulfone motif in drug design and discovery. |
| AID1369463 | Fungicidal activity against fluconazole-resistant Candida albicans 56214 after 96 hrs | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9 | Combating Drug-Resistant Fungi with Novel Imperfectly Amphipathic Palindromic Peptides. |
| AID1379937 | Antifungal activity against Candida glabrata clinical isolates assessed as inhibition of microbial growth incubated for 24 hrs by broth microdilution method | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Synthesis, biological evaluation and quantitative structure-active relationships of 1,3-thiazolidin-4-one derivatives. A promising chemical scaffold endowed with high antifungal potency and low cytotoxicity. |
| AID1369465 | Fungicidal activity against fluconazole-resistant Candida albicans 17546 after 96 hrs | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9 | Combating Drug-Resistant Fungi with Novel Imperfectly Amphipathic Palindromic Peptides. |
| AID1781971 | Inhibition of CYP3A4T in human liver microsomes using midazolam as substrate incubated for 10 mins in presence of NADPH by LC-MS/MS analysis | 2021 | Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21 | Discovery of 1-Amino-1 |
| AID1403678 | Antifungal activity against Aspergillus niger assessed as diameter of inhibition zone at 100 ug/well after 48 hrs by agar well diffusion method | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Synthesis and antimicrobial activity of pyrimidinyl 1,3,4-oxadiazoles, 1,3,4-thiadiazoles and 1,2,4-triazoles. |
| AID1813640 | Inhibition of CYP3A4 in human liver microsome using midazolam as substrate | 2021 | Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23 | Synthesis, Characterization, and Preclinical Evaluation of a Small-Molecule Prostate-Specific Membrane Antigen-Targeted Monomethyl Auristatin E Conjugate. |
| AID1833887 | Inhibition of Naegleria fowleri CYP51 catalytic activity using [3-3H]sterol substrate measured after 1 hr by RP-HPLC analysis | 2021 | Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23 | Relaxed Substrate Requirements of Sterol 14α-Demethylase from |
| AID1402207 | Antifungal activity against Penicillium chrysogenum assessed as zone of inhibition at 50 ug/well after 48 hrs by agar well diffusion method | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Green approach for the synthesis of thiophenyl pyrazoles and isoxazoles by adopting 1,3-dipolar cycloaddition methodology and their antimicrobial activity. |
| AID1864895 | Antifungal activity against fluconazole -resistant Candida albicans 904 assessed as fungal growth inhibition measured after 72 hrs by double dilution method | |||
| AID1890719 | Inhibition of human CYP3A4 at 10 uM incubated for 20 mins in presence of NADPH regenerating system by luminescence assay relative to control | 2022 | Bioorganic & medicinal chemistry letters, 05-15, Volume: 64 | Enteroviral replication inhibition by N-Alkyl triazolopyrimidinone derivatives through a non-capsid binding mode. |
| AID1882214 | Antifungal activity against Valsa mali | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Natural and synthetic β-carboline as a privileged antifungal scaffolds. |
| AID1578457 | Fraction unbound in Wistar Han rat white adipose tissue at 2 uM incubated for 6 hrs by equilibrium dialysis method | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Structural attributes influencing unbound tissue distribution. |
| AID1729758 | Antifungal activity against Candida albicans isolate 11 assessed as reduction in fungal growth incubated for 48 hrs by broth microdilution method | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Design, synthesis, and biodistribution studies of new analogues of marine alkaloids: Potent in vitro and in vivo fungicidal agents against Candida spp. |
| AID1497278 | Selectivity index, ratio of IC50 for CYP19 (unknown origin) to IC50 for recombinant CYP17 (unknown origin) | 2018 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 28, Issue:13 | Design and synthesis of functionalized piperazin-1yl-(E)-stilbenes as inhibitors of 17α-hydroxylase-C17,20-lyase (Cyp17). |
| AID1816739 | Inhibition of CYP3A4 (unknown origin) at 0.1 uM using testosterone as substrate relative to control | 2021 | European journal of medicinal chemistry, Aug-05, Volume: 220 | Design, synthesis, and biological evaluation of novel dual inhibitors targeting lysine specific demethylase 1 (LSD1) and histone deacetylases (HDAC) for treatment of gastric cancer. |
| AID1596684 | Antifungal activity against Aspergillus fumigatus ATCC 1022 after 72 hrs by microdilution technique | 2019 | European journal of medicinal chemistry, Aug-01, Volume: 175 | Appendix A. dithioloquinolinethiones as new potential multitargeted antibacterial and antifungal agents: Synthesis, biological evaluation and molecular docking studies. |
| AID1882216 | Antifungal activity against Alternaria brassicae | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Natural and synthetic β-carboline as a privileged antifungal scaffolds. |
| AID1901577 | Inhibition of CYP3A4M in human liver microsomes in presence of NADPH incubated for 3 to 20 mins by LC-MS/MS analysis | 2022 | Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5 | Discovery of Novel Bicyclic Imidazolopyridine-Containing Human Urate Transporter 1 Inhibitors as Hypouricemic Drug Candidates with Improved Efficacy and Favorable Druggability. |
| AID1596699 | Fungicidal activity against Penicillium verrucosum var. cyclopium food isolate incubated for 72 hrs followed by sub-culturing on broth malt medium and measured after 72 hrs | 2019 | European journal of medicinal chemistry, Aug-01, Volume: 175 | Appendix A. dithioloquinolinethiones as new potential multitargeted antibacterial and antifungal agents: Synthesis, biological evaluation and molecular docking studies. |
| AID1729748 | Antifungal activity against Candida albicans isolate 1 assessed as reduction in fungal growth incubated for 48 hrs by broth microdilution method | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Design, synthesis, and biodistribution studies of new analogues of marine alkaloids: Potent in vitro and in vivo fungicidal agents against Candida spp. |
| AID1729764 | Fungicidal activity against Candida krusei ATCC 34135 assessed as fungal killing incubated for 48 hrs followed by plating on SD agar plate | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Design, synthesis, and biodistribution studies of new analogues of marine alkaloids: Potent in vitro and in vivo fungicidal agents against Candida spp. |
| AID1634152 | Lipophilicity, log D of compound at pH 7.4 | 2019 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16 | Strategies for the development of highly selective cytochrome P450 inhibitors: Several CYP targets in current research. |
| AID1347596 | Inhibition of aromatase (unknown origin) using O-benzyl fluorescein benzyl ester as substrate in presence of NADPH-generating system by fluorescence assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Synthesis, molecular docking, and QSAR study of sulfonamide-based indoles as aromatase inhibitors. |
| AID1402885 | Cytotoxicity against mouse NIH/3T3 cells assessed as reduction in cell viability after 24 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | The synthesis, antifungal and apoptotic effects of triazole-oxadiazoles against Candida species. |
| AID1860408 | Inhibition of CYP3A4 in human liver microsomes at 10 uM preincubated for 10 mins followed by addition of NADPH-regenerating system and measured after 15 mins by LC-MS/MS analysis relative to control | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Design, synthesis, and biological evaluation of novel pyrazolo [3,4-d]pyrimidine derivatives as potent PLK4 inhibitors for the treatment of TRIM37-amplified breast cancer. |
| AID1529090 | Binding affinity to heme in His-tagged CYP3A5 (unknown origin) expressed in Escherichia coli DH5alpha assessed as changes in absorbance spectra of heme-compound complex by measuring dissociation constant by UV-vis spectrophotometric titration analysis | 2020 | Journal of medicinal chemistry, 02-13, Volume: 63, Issue:3 | Clobetasol Propionate Is a Heme-Mediated Selective Inhibitor of Human Cytochrome P450 3A5. |
| AID1369489 | Antifungal activity against Candida albicans cgmcc 2.2086 in presence of 50% human heat-inactivated serum by broth dilution method | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9 | Combating Drug-Resistant Fungi with Novel Imperfectly Amphipathic Palindromic Peptides. |
| AID1636386 | Drug activation in human Hep3B cells assessed as human CYP3A4-mediated drug metabolism-induced cytotoxicity measured as decrease in cell viability at 46.2 uM pre-incubated with BSO for 18 hrs followed by incubation with compound for 3 hrs in presence of N | 2016 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16 | Development of a cell viability assay to assess drug metabolite structure-toxicity relationships. |
| AID1729747 | Antifungal activity against Candida tropicalis ATCC 28707 assessed as reduction in fungal growth incubated for 48 hrs by broth microdilution method | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Design, synthesis, and biodistribution studies of new analogues of marine alkaloids: Potent in vitro and in vivo fungicidal agents against Candida spp. |
| AID1484688 | Antileishmanial activity against Leishmania amazonensis LV78 promastigotes forms after 8 days | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | An overview of azoles targeting sterol 14α-demethylase for antileishmanial therapy. |
| AID1729743 | Antifungal activity against Candida albicans ATCC 10231 assessed as reduction in fungal growth incubated for 48 hrs by broth microdilution method | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Design, synthesis, and biodistribution studies of new analogues of marine alkaloids: Potent in vitro and in vivo fungicidal agents against Candida spp. |
| AID1864877 | Antifungal activity against Candida albicans ATCC SC5314 assessed as fungal growth inhibition measured after 72 hrs by double dilution method | |||
| AID1674184 | Toxicity in po dosed human assessed as maximum daily dose | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20 | Drug Induced Liver Injury (DILI). Mechanisms and Medicinal Chemistry Avoidance/Mitigation Strategies. |
| AID1369456 | Fungicidal activity against Candida albicans cgmcc 2.2086 after 96 hrs | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9 | Combating Drug-Resistant Fungi with Novel Imperfectly Amphipathic Palindromic Peptides. |
| AID1537284 | Antifungal activity against Botrytis cinerea Pers. after 3 to 7 days by microbroth dilution method | 2019 | Journal of natural products, 02-22, Volume: 82, Issue:2 | Prenylated Indole Diterpene Alkaloids from a Mine-Soil-Derived Tolypocladium sp. |
| AID1596688 | Antifungal activity against Aspergillus ochraceus ATCC 12066 after 72 hrs by microdilution technique | 2019 | European journal of medicinal chemistry, Aug-01, Volume: 175 | Appendix A. dithioloquinolinethiones as new potential multitargeted antibacterial and antifungal agents: Synthesis, biological evaluation and molecular docking studies. |
| AID1529075 | Inhibition of CYP3A5 in lentiviral pLVX-TRE3G-ZsGreen1-CYP3A5 transduced wild type human AsPC1 cells overexpressing CYP3A5 assessed as decrease in 1-hydroxymidazolam formation using midazolam as substrate after 24 hrs by LC-MS/MS analysis | 2020 | Journal of medicinal chemistry, 02-13, Volume: 63, Issue:3 | Clobetasol Propionate Is a Heme-Mediated Selective Inhibitor of Human Cytochrome P450 3A5. |
| AID1369449 | Antifungal activity against fluconazole-resistant Candida albicans 56452 after 48 hrs by broth microdilution method | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9 | Combating Drug-Resistant Fungi with Novel Imperfectly Amphipathic Palindromic Peptides. |
| AID1729751 | Antifungal activity against Candida albicans isolate 4 assessed as reduction in fungal growth incubated for 48 hrs by broth microdilution method | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Design, synthesis, and biodistribution studies of new analogues of marine alkaloids: Potent in vitro and in vivo fungicidal agents against Candida spp. |
| AID1729746 | Antifungal activity against Candida krusei ATCC 34135 assessed as reduction in fungal growth incubated for 48 hrs by broth microdilution method | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Design, synthesis, and biodistribution studies of new analogues of marine alkaloids: Potent in vitro and in vivo fungicidal agents against Candida spp. |
| AID1537283 | Antifungal activity against Alternaria alternata after 3 to 7 days by microbroth dilution method | 2019 | Journal of natural products, 02-22, Volume: 82, Issue:2 | Prenylated Indole Diterpene Alkaloids from a Mine-Soil-Derived Tolypocladium sp. |
| AID1729749 | Antifungal activity against Candida albicans isolate 2 assessed as reduction in fungal growth incubated for 48 hrs by broth microdilution method | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Design, synthesis, and biodistribution studies of new analogues of marine alkaloids: Potent in vitro and in vivo fungicidal agents against Candida spp. |
| AID1328453 | Inhibition of human Cyp3A4 using testosterone as substrate by LC-MS/MS analysis | 2016 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 26, Issue:23 | Design, synthesis, and evaluation of (2S,4R)-Ketoconazole sulfonamide analogs as potential treatments for Metabolic Syndrome. |
| AID1918340 | Antifungal activity against fluconazole-resistant Candida albicans 901 assessed as inhibition of fungal growth measured after 72 hrs by CLSI based liquid medium dilution method | 2022 | Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21 | Novel Aryl Alkamidazole Derivatives as Multifunctional Antifungal Inhibitors: Design, Synthesis, and Biological Evaluation. |
| AID1527675 | Inhibition of CYP3A4 in pooled human liver microsomes pre-incubated for 5 mins before NADPH addition and measured after 10 mins by UPLC-MS/MS analysis relative to control | 2019 | Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23 | Discovery and Characterization of Potent Pan-Genotypic HCV NS5A Inhibitors Containing Novel Tricyclic Central Core Leading to Clinical Candidate. |
| AID1529078 | Inhibition of CYP3A4 in CRISPR/Cas9-mediated CYP3A5 knock-out and doxycycline-induced CYP3A4 overexpressing human AsPC1 cells assessed as decrease in 1-hydroxymidazolam formation using midazolam as substrate pretreated with doxycycline for 24 hrs followed | 2020 | Journal of medicinal chemistry, 02-13, Volume: 63, Issue:3 | Clobetasol Propionate Is a Heme-Mediated Selective Inhibitor of Human Cytochrome P450 3A5. |
| AID1411637 | Fungicidal activity against Aspergillus versicolor ATCC 11730 incubated for 72 hrs followed by serial sub-cultivation for 72 hrs and measured after 72 hrs by serial dilution method | |||
| AID1596689 | Fungicidal activity against Aspergillus ochraceus ATCC 12066 incubated for 72 hrs followed by sub-culturing on broth malt medium and measured after 72 hrs | 2019 | European journal of medicinal chemistry, Aug-01, Volume: 175 | Appendix A. dithioloquinolinethiones as new potential multitargeted antibacterial and antifungal agents: Synthesis, biological evaluation and molecular docking studies. |
| AID1369464 | Fungicidal activity against Candida albicans 14936 after 96 hrs | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9 | Combating Drug-Resistant Fungi with Novel Imperfectly Amphipathic Palindromic Peptides. |
| AID1571586 | Bactericidal activity against Trichophyton mentagrophytes var. granulosum 1773 measured after 4 hrs | 2018 | MedChemComm, Dec-01, Volume: 9, Issue:12 | Design, synthesis, and biological activity of novel ammonium salts containing sterically hindered phenolic fragment and phosphoryl group. |
| AID1818561 | Cytotoxicity in human MES-SA/Dx5 cells assessed as reduction in cell viability at 1.28 uM incubated for 3 days by MTT assay relative to control | 2022 | Journal of medicinal chemistry, 01-13, Volume: 65, Issue:1 | Discovery and Characterization of Potent Dual P-Glycoprotein and CYP3A4 Inhibitors: Design, Synthesis, Cryo-EM Analysis, and Biological Evaluations. |
| AID1546158 | Antimicrobial activity against Pseudomonas aeruginosa assessed as zone of inhibition at 10 ug/ml | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | Current scenario of tetrazole hybrids for antibacterial activity. |
| AID1402883 | Antifungal activity against Candida krusei ATCC 6258 by broth microdilution assay | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | The synthesis, antifungal and apoptotic effects of triazole-oxadiazoles against Candida species. |
| AID1399519 | Antifungal activity against Penicillium ochrochloron ATCC 9112 after 72 hrs by serial dilution assay | 2018 | Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16 | 5-Adamantan thiadiazole-based thiazolidinones as antimicrobial agents. Design, synthesis, molecular docking and evaluation. |
| AID1379940 | Antifungal activity against Candida parapsilosis clinical isolates assessed as inhibition of microbial growth incubated for 24 hrs by broth microdilution method | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Synthesis, biological evaluation and quantitative structure-active relationships of 1,3-thiazolidin-4-one derivatives. A promising chemical scaffold endowed with high antifungal potency and low cytotoxicity. |
| AID1721982 | Antifungal activity Aspergillus versicolor by microdilution method | 2020 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 30, Issue:17 | New vinyl-1,2,4-triazole derivatives as antimicrobial agents: Synthesis, biological evaluation and molecular docking studies. |
| AID1769162 | Inhibition of CYP1A2 in human liver microsomes assessed as remaining activity at 1 to 10 uM using phenacetin as substrate preincubated for 5 mins followed by addition of NADPH generation system for 15 mins by LC-MS/MS analysis | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | Discovery of G Protein-Biased Antagonists against 5-HT |
| AID1350706 | Apparent permeability cross basolateral to apical side in MDCK-MDR1 cells at 5 uM after 90 mins by LC-MS/MS analysis | 2018 | Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14 | Optimization of Isothiazolo[4,3- b]pyridine-Based Inhibitors of Cyclin G Associated Kinase (GAK) with Broad-Spectrum Antiviral Activity. |
| AID1365625 | Antileishmanial activity against Leishmania amazonensis amastigotes assessed as reduction in bacterial lode in late log phase after 24 hrs | 2017 | Bioorganic & medicinal chemistry, 11-01, Volume: 25, Issue:21 | Recently reported biological activities of pyrazole compounds. |
| AID1721986 | Antifungal activity Penicillium funiculosum by microdilution method | 2020 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 30, Issue:17 | New vinyl-1,2,4-triazole derivatives as antimicrobial agents: Synthesis, biological evaluation and molecular docking studies. |
| AID1369451 | Antifungal activity against Candida albicans 14936 after 48 hrs by broth microdilution method | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9 | Combating Drug-Resistant Fungi with Novel Imperfectly Amphipathic Palindromic Peptides. |
| AID1369454 | Antifungal activity against Candida krusei cgmcc 2.1857 after 48 hrs by broth microdilution method | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9 | Combating Drug-Resistant Fungi with Novel Imperfectly Amphipathic Palindromic Peptides. |
| AID1678799 | Antimalarial activity against chloroquine resistant Plasmodium falciparum | 2020 | RSC medicinal chemistry, Feb-01, Volume: 11, Issue:2 | An epigrammatic status of the ' |
| AID1412890 | Inhibition of recombinant human CYP3A4 by bioluminescence method | 2018 | MedChemComm, Jun-01, Volume: 9, Issue:6 | Tricyclic xanthine derivatives containing a basic substituent: adenosine receptor affinity and drug-related properties. |
| AID1595158 | Inhibition of human CYP3A4 measured after 30 mins in presence of NADPH regeneration system by luminescent CYP3A4 P450-Glo assay | |||
| AID1369448 | Antifungal activity against Candida albicans isolated from alveolar fluid after 48 hrs by broth microdilution method | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9 | Combating Drug-Resistant Fungi with Novel Imperfectly Amphipathic Palindromic Peptides. |
| AID1676915 | Aggregation property of the compound in PBS buffer assessed as aggregate formation at 10 to 100 uM incubated for 2 hrs by light scattering spectrofluorimetric assay | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20 | Glucosylpolyphenols as Inhibitors of Aβ-Induced Fyn Kinase Activation and Tau Phosphorylation: Synthesis, Membrane Permeability, and Exploratory Target Assessment within the Scope of Type 2 Diabetes and Alzheimer's Disease. |
| AID1369533 | Antifungal activity against Candida albicans 58288 after 48 hrs by broth microdilution method | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9 | Combating Drug-Resistant Fungi with Novel Imperfectly Amphipathic Palindromic Peptides. |
| AID1369445 | Antifungal activity against Candida albicans SP3903 after 48 hrs by broth microdilution method | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9 | Combating Drug-Resistant Fungi with Novel Imperfectly Amphipathic Palindromic Peptides. |
| AID1596685 | Fungicidal activity against Aspergillus fumigatus ATCC 1022 incubated for 72 hrs followed by sub-culturing on broth malt medium and measured after 72 hrs | 2019 | European journal of medicinal chemistry, Aug-01, Volume: 175 | Appendix A. dithioloquinolinethiones as new potential multitargeted antibacterial and antifungal agents: Synthesis, biological evaluation and molecular docking studies. |
| AID1771188 | Inhibition of CYP3A4 (unknown origin) assessed as activity using midazolam as substrate at 0.03 uM relative to control | 2021 | Journal of medicinal chemistry, 09-09, Volume: 64, Issue:17 | Discovery of |
| AID1729750 | Antifungal activity against Candida albicans isolate 3 assessed as reduction in fungal growth incubated for 48 hrs by broth microdilution method | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Design, synthesis, and biodistribution studies of new analogues of marine alkaloids: Potent in vitro and in vivo fungicidal agents against Candida spp. |
| AID1574940 | Inhibition of CYP2C8 in human liver microsomes assessed as residual activity at 10 uM using amiodiaquine as substrate preincubated for 5 mins followed by NADPH addition and measured after 15 mins by LC-MS/MS analysis relative to control | 2019 | Bioorganic & medicinal chemistry letters, 02-01, Volume: 29, Issue:3 | Click chemistry for improvement in selectivity of quinazoline-based kinase inhibitors for mutant epidermal growth factor receptors. |
| AID1652318 | Protein binding in plasma (unknown origin) | 2020 | Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13 | Novel Pyrrolopyridone Bromodomain and Extra-Terminal Motif (BET) Inhibitors Effective in Endocrine-Resistant ER+ Breast Cancer with Acquired Resistance to Fulvestrant and Palbociclib. |
| AID1546118 | Antimicrobial activity against Staphylococcus aureus assessed as zone of inhibition at 250 ug/ml | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | Current scenario of tetrazole hybrids for antibacterial activity. |
| AID1369447 | Antifungal activity against Candida albicans SP3876 after 48 hrs by broth microdilution method | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9 | Combating Drug-Resistant Fungi with Novel Imperfectly Amphipathic Palindromic Peptides. |
| AID1595233 | Antifungal activity against Aspergillus fumigatus assessed as reduction in fungal cell viability by broth dilution method | 2019 | European journal of medicinal chemistry, Jun-01, Volume: 171 | Insights into the chemistry and therapeutic potential of furanones: A versatile pharmacophore. |
| AID1880386 | Inhibition of CYP3A4 in human liver microsomes using midazolam as substrate incubated for 15 to 45 mins in presence of NADPH | 2022 | Journal of medicinal chemistry, 06-23, Volume: 65, Issue:12 | Structure-Based Discovery of Novel NH |
| AID1379939 | Antifungal activity against Candida krusei clinical isolates assessed as inhibition of microbial growth incubated for 24 hrs by broth microdilution method | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Synthesis, biological evaluation and quantitative structure-active relationships of 1,3-thiazolidin-4-one derivatives. A promising chemical scaffold endowed with high antifungal potency and low cytotoxicity. |
| AID1882215 | Antifungal activity against Alternaria alternata | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Natural and synthetic β-carboline as a privileged antifungal scaffolds. |
| AID1411642 | Antifungal activity against Trichoderma viride IAM 5061 after 72 hrs by serial dilution method | |||
| AID1402882 | Antifungal activity against Candida glabrata ATCC 90030 by broth microdilution assay | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | The synthesis, antifungal and apoptotic effects of triazole-oxadiazoles against Candida species. |
| AID1764880 | Inhibition of CYP2C19 (unknown origin) assessed as enzyme residual activity at 10 uM | 2021 | European journal of medicinal chemistry, Jun-05, Volume: 218 | Discovery of novel potent migrastatic Thiazolo[5,4-b]pyridines targeting Lysyl-tRNA synthetase (KRS) for treatment of Cancer metastasis. |
| AID1652093 | Antifungal activity against Candida albicans assessed as reduction in microbial growth | 2020 | Journal of natural products, 04-24, Volume: 83, Issue:4 | Microketides A and B, Polyketides from a Gorgonian-Derived |
| AID1711075 | Inhibition of human CYP3A4 at 20 to 200 uM measured after 15 mins relative to control | 2016 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 26, Issue:3 | In vitro synergistic anticancer activity of the combination of T-type calcium channel blocker and chemotherapeutic agent in A549 cells. |
| AID1729771 | Fungicidal activity against Candida albicans isolate 6 assessed as fungal killing incubated for 48 hrs followed by plating on SD agar plate | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Design, synthesis, and biodistribution studies of new analogues of marine alkaloids: Potent in vitro and in vivo fungicidal agents against Candida spp. |
| AID1578460 | Fraction unbound in Wistar Han rat liver at 2 uM incubated for 6 hrs by equilibrium dialysis method | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Structural attributes influencing unbound tissue distribution. |
| AID1369462 | Fungicidal activity against fluconazole-resistant Candida albicans 56452 after 96 hrs | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9 | Combating Drug-Resistant Fungi with Novel Imperfectly Amphipathic Palindromic Peptides. |
| AID1721994 | Fungicidal activity Penicillium funiculosum | 2020 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 30, Issue:17 | New vinyl-1,2,4-triazole derivatives as antimicrobial agents: Synthesis, biological evaluation and molecular docking studies. |
| AID1537338 | Antifungal activity against Alternaria brassicicola CICC 2646 after 48 hrs by broth dilution assay | 2019 | Journal of natural products, 02-22, Volume: 82, Issue:2 | Absolute Configuration of Bioactive Azaphilones from the Marine-Derived Fungus Pleosporales sp. CF09-1. |
| AID1402901 | Induction of apoptosis in Candida parapsilosis ATCC 22019 assessed as necrotic cells at antifungal MIC90 after 24 hrs by Annexin V/propidium iodide staining based flow cytometry (Rvb = 1.4%) | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | The synthesis, antifungal and apoptotic effects of triazole-oxadiazoles against Candida species. |
| AID1529092 | Inhibition of CYP3A4 in CRISPR/Cas9-mediated CYP3A5 knock-out and doxycycline-induced CYP3A4 overexpressing human AsPC1 cells assessed as decrease in 1-hydroxymidazolam formation using midazolam as substrate at 1 uM pretreated with doxycycline for 24 hrs | 2020 | Journal of medicinal chemistry, 02-13, Volume: 63, Issue:3 | Clobetasol Propionate Is a Heme-Mediated Selective Inhibitor of Human Cytochrome P450 3A5. |
| AID1529083 | Cytotoxicity against CRISPR/Cas9-mediated CYP3A5 knock-out and lentiviral pLVX-TRE3G-ZsGreen1-CYP3A4 transduced human AsPC1 cells overexpressing CYP3A4 assessed as cell growth | 2020 | Journal of medicinal chemistry, 02-13, Volume: 63, Issue:3 | Clobetasol Propionate Is a Heme-Mediated Selective Inhibitor of Human Cytochrome P450 3A5. |
| AID1537286 | Antifungal activity against Verticillium dahliae Kleb after 3 to 7 days by microbroth dilution method | 2019 | Journal of natural products, 02-22, Volume: 82, Issue:2 | Prenylated Indole Diterpene Alkaloids from a Mine-Soil-Derived Tolypocladium sp. |
| AID1574943 | Inhibition of CYP2D6 in human liver microsomes assessed as residual activity at 10 uM using dextromethorphan as substrate preincubated for 5 mins followed by NADPH addition and measured after 15 mins by LC-MS/MS analysis relative to control | 2019 | Bioorganic & medicinal chemistry letters, 02-01, Volume: 29, Issue:3 | Click chemistry for improvement in selectivity of quinazoline-based kinase inhibitors for mutant epidermal growth factor receptors. |
| AID1721981 | Antifungal activity Aspergillus fumigatus by microdilution method | 2020 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 30, Issue:17 | New vinyl-1,2,4-triazole derivatives as antimicrobial agents: Synthesis, biological evaluation and molecular docking studies. |
| AID1918338 | Antifungal activity against fluconazole-resistant Candida albicans CaR assessed as inhibition of fungal growth measured after 72 hrs by CLSI based liquid medium dilution method | 2022 | Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21 | Novel Aryl Alkamidazole Derivatives as Multifunctional Antifungal Inhibitors: Design, Synthesis, and Biological Evaluation. |
| AID1822292 | Inhibition of CYP3A4M in human liver microsomes using midazolam as substrate incubated for 15 to 45 mins in presence of NADPH | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 | Discovery of Novel Pyridine-Dimethyl-Phenyl-DAPY Hybrids by Molecular Fusing of Methyl-Pyrimidine-DAPYs and Difluoro-Pyridinyl-DAPYs: Improving the Druggability toward High Inhibitory Activity, Solubility, Safety, and PK. |
| AID1578472 | Unbound tissue partition coefficient, ratio of drug level in skeletal muscle to plasma in Wistar Han rat at 1 to 2 mg/kg, iv infused for 10 to 20 hrs by LC-MS/MS analysis | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Structural attributes influencing unbound tissue distribution. |
| AID1636445 | Drug activation in human Hep3B cells assessed as human CYP2D6-mediated drug metabolism-induced cytotoxicity measured as decrease in cell viability at 96.1 uM pre-incubated with BSO for 18 hrs followed by incubation with compound for 3 hrs in presence of N | 2016 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16 | Development of a cell viability assay to assess drug metabolite structure-toxicity relationships. |
| AID1764881 | Inhibition of CYP3A4 (unknown origin) assessed as enzyme residual activity at 10 uM | 2021 | European journal of medicinal chemistry, Jun-05, Volume: 218 | Discovery of novel potent migrastatic Thiazolo[5,4-b]pyridines targeting Lysyl-tRNA synthetase (KRS) for treatment of Cancer metastasis. |
| AID1756369 | Inhibition of CYP3A4/5 in human liver microsomes using Midazolam as substrate measured after 20 mins by LC-MS/MS analysis | 2021 | European journal of medicinal chemistry, Mar-05, Volume: 213 | Discovery and development of novel pyrimidine and pyrazolo/thieno-fused pyrimidine derivatives as potent and orally active inducible nitric oxide synthase dimerization inhibitor with efficacy for arthritis. |
| AID1529085 | Cytotoxicity against CRISPR/Cas9-mediated CYP3A5 knock-out and doxycycline-induced CYP3A4 overexpressing human AsPC1 cells assessed as cell growth | 2020 | Journal of medicinal chemistry, 02-13, Volume: 63, Issue:3 | Clobetasol Propionate Is a Heme-Mediated Selective Inhibitor of Human Cytochrome P450 3A5. |
| AID1369452 | Antifungal activity against fluconazole-resistant Candida albicans 17546 after 48 hrs by broth microdilution method | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9 | Combating Drug-Resistant Fungi with Novel Imperfectly Amphipathic Palindromic Peptides. |
| AID1546120 | Antimicrobial activity against Escherichia coli assessed as zone of inhibition at 250 ug/ml | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | Current scenario of tetrazole hybrids for antibacterial activity. |
| AID1872790 | Antifungal activity against Aspergillus niger assessed as zone of inhibition | 2022 | European journal of medicinal chemistry, Apr-15, Volume: 234 | Recent applications of vinyl sulfone motif in drug design and discovery. |
| AID1537282 | Antifungal activity against Corynespora cassiicola after 3 to 7 days by microbroth dilution method | 2019 | Journal of natural products, 02-22, Volume: 82, Issue:2 | Prenylated Indole Diterpene Alkaloids from a Mine-Soil-Derived Tolypocladium sp. |
| AID1574944 | Inhibition of CYP2E1 in human liver microsomes assessed as residual activity at 10 uM using chlorzoxazone as substrate preincubated for 5 mins followed by NADPH addition and measured after 15 mins by LC-MS/MS analysis relative to control | 2019 | Bioorganic & medicinal chemistry letters, 02-01, Volume: 29, Issue:3 | Click chemistry for improvement in selectivity of quinazoline-based kinase inhibitors for mutant epidermal growth factor receptors. |
| AID1411643 | Fungicidal activity against Trichoderma viride IAM 5061 incubated for 72 hrs followed by serial sub-cultivation for 72 hrs and measured after 72 hrs by serial dilution method | |||
| AID1412938 | Antifungal activity against Aspergillus niger by microdilution method | 2018 | MedChemComm, May-01, Volume: 9, Issue:5 | Design, synthesis and antimicrobial activity of usnic acid derivatives. |
| AID1546105 | Antimicrobial activity against Bacillus subtilis | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | Current scenario of tetrazole hybrids for antibacterial activity. |
| AID1729763 | Fungicidal activity against Candida glabrata ATCC 2001 assessed as fungal killing incubated for 48 hrs followed by plating on SD agar plate | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Design, synthesis, and biodistribution studies of new analogues of marine alkaloids: Potent in vitro and in vivo fungicidal agents against Candida spp. |
| AID1399524 | Fungicidal activity against Penicillium cyclopium var verucosum after 144 hrs by serial dilution assay | 2018 | Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16 | 5-Adamantan thiadiazole-based thiazolidinones as antimicrobial agents. Design, synthesis, molecular docking and evaluation. |
| AID1833385 | Inhibition of human CYP3A4 preincubated for 10 mins followed by substrate and NADP addition measured after 30 mins by fluorescence assay | |||
| AID1574945 | Inhibition of CYP3A4 in human liver microsomes assessed as residual activity at 10 uM using midazolam as substrate preincubated for 5 mins followed by NADPH addition and measured after 15 mins by LC-MS/MS analysis relative to control | 2019 | Bioorganic & medicinal chemistry letters, 02-01, Volume: 29, Issue:3 | Click chemistry for improvement in selectivity of quinazoline-based kinase inhibitors for mutant epidermal growth factor receptors. |
| AID1399516 | Fungicidal activity against Trichoderma viride IAM 5061 after 144 hrs by serial dilution assay | 2018 | Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16 | 5-Adamantan thiadiazole-based thiazolidinones as antimicrobial agents. Design, synthesis, molecular docking and evaluation. |
| AID1529098 | Binding affinity to His-tagged CYP3A5 (unknown origin) expressed in Escherichia coli DH5alpha assessed as induction of new LS formation by EPR spectroscopy | 2020 | Journal of medicinal chemistry, 02-13, Volume: 63, Issue:3 | Clobetasol Propionate Is a Heme-Mediated Selective Inhibitor of Human Cytochrome P450 3A5. |
| AID1402890 | Induction of apoptosis in Candida glabrata ATCC 90030 assessed as live cells at antifungal MIC90 after 24 hrs by Annexin V/propidium iodide staining based flow cytometry (Rvb = 99.5%) | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | The synthesis, antifungal and apoptotic effects of triazole-oxadiazoles against Candida species. |
| AID1729777 | Fungicidal activity against Candida albicans isolate 12 assessed as fungal killing incubated for 48 hrs followed by plating on SD agar plate | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Design, synthesis, and biodistribution studies of new analogues of marine alkaloids: Potent in vitro and in vivo fungicidal agents against Candida spp. |
| AID1783793 | Inhibition of CYP3A4 in human liver microsome using Nifedipine as a substrate incubated for 10 mins in the presence of NADPH by LC-MS/MS analysis | 2021 | European journal of medicinal chemistry, Nov-15, Volume: 224 | Improving the metabolic stability of antifungal compounds based on a scaffold hopping strategy: Design, synthesis, and structure-activity relationship studies of dihydrooxazole derivatives. |
| AID1399520 | Fungicidal activity against Penicillium ochrochloron ATCC 9112 after 144 hrs by serial dilution assay | 2018 | Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16 | 5-Adamantan thiadiazole-based thiazolidinones as antimicrobial agents. Design, synthesis, molecular docking and evaluation. |
| AID1411647 | Antifungal activity against Candida albicans after 72 hrs by serial dilution method | |||
| AID1895934 | Inhibition of CYP3A4M in human liver microsomes incubated for 20 mins in presence of NADPH by LC-MS/MS analysis | 2021 | Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24 | Identification of C5-NH |
| AID1918333 | Antifungal activity against Cryptococcus neoformans assessed as inhibition of fungal growth measured after 72 hrs by CLSI based liquid medium dilution method | 2022 | Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21 | Novel Aryl Alkamidazole Derivatives as Multifunctional Antifungal Inhibitors: Design, Synthesis, and Biological Evaluation. |
| AID1772932 | Inhibition of CYP3A4 (unknown origin) using BOMCC as a substrate incubated for 20 mins by fluorescence based analysis | 2021 | European journal of medicinal chemistry, Nov-15, Volume: 224 | Discovery of first-in-class imidazothiazole-based potent and selective ErbB4 (HER4) kinase inhibitors. |
| AID1388199 | Antifungal activity against Aspergillus niger ATCC 9029 at 100 ug/ml incubated for 72 hrs by agar disc diffusion assay | 2017 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 27, Issue:18 | Synthesis, antimicrobial activity, structure-activity relationship and cytotoxic studies of a new series of functionalized (Z)-3-(2-oxo-2-substituted ethylidene)-3,4-dihydro-2H-benzo[b][1,4]oxazin-2-ones. |
| AID1379465 | Inhibition of CYP3A4 (unknown origin) | 2017 | ACS medicinal chemistry letters, Aug-10, Volume: 8, Issue:8 | 1-Benzyl-3-aryl-2-thiohydantoin Derivatives as New Anti- |
| AID1769165 | Metabolic stability in human liver microsomes assessed as parent compound remaining at 1 uM preincubated for 5 mins followed by NADPH regeneration system addition and measured after 30 mins by LC-MS analysis | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | Discovery of G Protein-Biased Antagonists against 5-HT |
| AID1595106 | Antifungal activity against Aspergillus niger assessed as inhibition zone at 50 ug/ml by disk diffusion method | 2019 | European journal of medicinal chemistry, May-15, Volume: 170 | Tetrazole hybrids and their antifungal activities. |
| AID1729754 | Antifungal activity against Candida albicans isolate 7 assessed as reduction in fungal growth incubated for 48 hrs by broth microdilution method | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Design, synthesis, and biodistribution studies of new analogues of marine alkaloids: Potent in vitro and in vivo fungicidal agents against Candida spp. |
| AID1861993 | Inhibition of CYP2D6 (unknown origin) using EOMCC as a substrate | 2022 | Bioorganic & medicinal chemistry, 09-01, Volume: 69 | Design, synthesis, and biological evaluation of a new series of pyrazole derivatives: Discovery of potent and selective JNK3 kinase inhibitors. |
| AID1578471 | Unbound tissue partition coefficient, ratio of drug level in liver to plasma in Wistar Han rat at 1 to 2 mg/kg, iv infused for 10 to 20 hrs by LC-MS/MS analysis | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Structural attributes influencing unbound tissue distribution. |
| AID1403680 | Antifungal activity against Penicillium chrysogenum assessed as diameter of inhibition zone at 25 ug/well after 48 hrs by agar well diffusion method | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Synthesis and antimicrobial activity of pyrimidinyl 1,3,4-oxadiazoles, 1,3,4-thiadiazoles and 1,2,4-triazoles. |
| AID1546160 | Antifungal activity against Aspergillus fumigatus assessed as zone of inhibition at 10 ug/ml | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | Current scenario of tetrazole hybrids for antibacterial activity. |
| AID1399521 | Antifungal activity against Candida albicans after 72 hrs by serial dilution assay | 2018 | Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16 | 5-Adamantan thiadiazole-based thiazolidinones as antimicrobial agents. Design, synthesis, molecular docking and evaluation. |
| AID1604268 | Inhibition of rat brain microsome HO-2 preincubated for 10 mins followed by beta-NADPH addition and measured after 15 mins by gas chromatography | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Heme Oxygenase-2 (HO-2) as a therapeutic target: Activators and inhibitors. |
| AID1832392 | Inhibition of CYP3A4 (unknown origin) using ketoconazole as substrate | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | Discovery of Novel Acetamide-Based Heme Oxygenase-1 Inhibitors with Potent |
| AID1402892 | Induction of apoptosis in Candida glabrata ATCC 90030 assessed as late apoptotic cells at antifungal MIC90 after 24 hrs by Annexin V/propidium iodide staining based flow cytometry (Rvb = 0.2%) | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | The synthesis, antifungal and apoptotic effects of triazole-oxadiazoles against Candida species. |
| AID1713219 | Cytotoxicity against Wistar rat PBMC assessed as inhibition of cell growth at 50 uM incubated for 24 hrs by sulforhodamine B assay relative to control | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Synthesis of 17β-N-arylcarbamoylandrost-4-en-3-one derivatives and their anti-proliferative effect on human androgen-sensitive LNCaP cell line. |
| AID1529077 | Inhibition of CYP3A5 in CRISPR/Cas9-mediated CYP3A5 knock-out and doxycycline-induced CYP3A5 overexpressing human AsPC1 cells assessed as decrease in 1-hydroxymidazolam formation using midazolam as substrate pretreated with doxycycline for 24 hrs followed | 2020 | Journal of medicinal chemistry, 02-13, Volume: 63, Issue:3 | Clobetasol Propionate Is a Heme-Mediated Selective Inhibitor of Human Cytochrome P450 3A5. |
| AID1403688 | Antifungal activity against Penicillium chrysogenum after 48 hrs by turbidity-based broth dilution assay | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Synthesis and antimicrobial activity of pyrimidinyl 1,3,4-oxadiazoles, 1,3,4-thiadiazoles and 1,2,4-triazoles. |
| AID1399515 | Antifungal activity against Trichoderma viride IAM 5061 after 72 hrs by serial dilution assay | 2018 | Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16 | 5-Adamantan thiadiazole-based thiazolidinones as antimicrobial agents. Design, synthesis, molecular docking and evaluation. |
| AID1721984 | Antifungal activity Aspergillus niger by microdilution method | 2020 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 30, Issue:17 | New vinyl-1,2,4-triazole derivatives as antimicrobial agents: Synthesis, biological evaluation and molecular docking studies. |
| AID1399514 | Fungicidal activity against Aspergillus niger ATCC 6275 after 144 hrs by serial dilution assay | 2018 | Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16 | 5-Adamantan thiadiazole-based thiazolidinones as antimicrobial agents. Design, synthesis, molecular docking and evaluation. |
| AID1399522 | Fungicidal activity against Candida albicans after 144 hrs by serial dilution assay | 2018 | Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16 | 5-Adamantan thiadiazole-based thiazolidinones as antimicrobial agents. Design, synthesis, molecular docking and evaluation. |
| AID1412950 | Fungicidal activity against Penicillium verrucosum var. cyclopium food isolate by microdilution method | 2018 | MedChemComm, May-01, Volume: 9, Issue:5 | Design, synthesis and antimicrobial activity of usnic acid derivatives. |
| AID1662850 | Antifungal activity against Trichophyton mentagrophytes | 2020 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 30, Issue:13 | Design and synthesis of amphiphilic 2-hydroxybenzylphosphonium salts with antimicrobial and antitumor dual action. |
| AID1388192 | Antifungal activity against Penicillium funiculosum ATCC 11797 incubated for 24 hrs by serial dilution method | 2017 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 27, Issue:18 | Synthesis, antimicrobial activity, structure-activity relationship and cytotoxic studies of a new series of functionalized (Z)-3-(2-oxo-2-substituted ethylidene)-3,4-dihydro-2H-benzo[b][1,4]oxazin-2-ones. |
| AID1662852 | Antifungal activity against Candida albicans | 2020 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 30, Issue:13 | Design and synthesis of amphiphilic 2-hydroxybenzylphosphonium salts with antimicrobial and antitumor dual action. |
| AID1764879 | Inhibition of CYP2C9 (unknown origin) assessed as enzyme residual activity at 10 uM | 2021 | European journal of medicinal chemistry, Jun-05, Volume: 218 | Discovery of novel potent migrastatic Thiazolo[5,4-b]pyridines targeting Lysyl-tRNA synthetase (KRS) for treatment of Cancer metastasis. |
| AID1546159 | Antimicrobial activity against Bacillus subtilis assessed as zone of inhibition at 10 ug/ml | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | Current scenario of tetrazole hybrids for antibacterial activity. |
| AID1864880 | Antifungal activity against Candida tropicalis ATCC 1369 assessed as fungal growth inhibition measured after 72 hrs by double dilution method | |||
| AID1864892 | Antifungal activity against fluconazole -resistant Candida albicans CaR assessed as fungal growth inhibition measured after 72 hrs by double dilution method | |||
| AID1402891 | Induction of apoptosis in Candida glabrata ATCC 90030 assessed as early apoptotic cells at antifungal MIC90 after 24 hrs by Annexin V/propidium iodide staining based flow cytometry (Rvb = 0%) | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | The synthesis, antifungal and apoptotic effects of triazole-oxadiazoles against Candida species. |
| AID1874022 | Inhibition of human CYP3A4 at 10 uM preincubated for 10 mins followed by NADPH addition and measured after 20 mins by luciferin reagent based luminescence analysis | 2022 | Bioorganic & medicinal chemistry, 08-15, Volume: 68 | Entry inhibition of hepatitis B virus using cyclosporin O derivatives with peptoid side chain incorporation. |
| AID1826368 | Inhibition of human recombinant CYP3A4 expressed in baculosomes by fluorescent homogenous assay | |||
| AID1402899 | Induction of apoptosis in Candida parapsilosis ATCC 22019 assessed as early apoptotic cells at antifungal MIC90 after 24 hrs by Annexin V/propidium iodide staining based flow cytometry (Rvb = 0.1%) | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | The synthesis, antifungal and apoptotic effects of triazole-oxadiazoles against Candida species. |
| AID1578468 | Unbound tissue partition coefficient, ratio of drug level in heart to plasma in Wistar Han rat at 1 to 2 mg/kg, iv infused for 10 to 20 hrs by LC-MS/MS analysis | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Structural attributes influencing unbound tissue distribution. |
| AID1350754 | Inhibition of recombinant human CYP3A4 in presence of NADPH generating system by fluorescence assay | 2018 | Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14 | Discovery of 5-Cyano-6-phenylpyrimidin Derivatives Containing an Acylurea Moiety as Orally Bioavailable Reversal Agents against P-Glycoprotein-Mediated Mutidrug Resistance. |
| AID1781972 | Inhibition of CYP3A4M in human liver microsomes using midazolam as substrate incubated for 10 mins in presence of NADPH by LC-MS/MS analysis | 2021 | Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21 | Discovery of 1-Amino-1 |
| AID1529082 | Cytotoxicity against doxycycline-induced CYP3A5 overexpressing wild type human AsPC1 cells assessed as cell growth | 2020 | Journal of medicinal chemistry, 02-13, Volume: 63, Issue:3 | Clobetasol Propionate Is a Heme-Mediated Selective Inhibitor of Human Cytochrome P450 3A5. |
| AID1703888 | Drug absorption of the compound incubated for 8 hrs by PAMPA-TGI assay | 2020 | European journal of medicinal chemistry, Oct-15, Volume: 204 | Discovery of sulfonyl hydrazone derivative as a new selective PDE4A and PDE4D inhibitor by lead-optimization approach on the prototype LASSBio-448: In vitro and in vivo preclinical studies. |
| AID1484709 | Antileishmanial activity against Leishmania major MRHO/IR/75/ER amastigote forms infected in mouse J774A.1 cells after 60 hrs by giemsa-staining based light microscopic analysis | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | An overview of azoles targeting sterol 14α-demethylase for antileishmanial therapy. |
| AID1369481 | Antifungal activity against Candida albicans cgmcc 2.2086 in presence of CaCl2 by broth dilution method | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9 | Combating Drug-Resistant Fungi with Novel Imperfectly Amphipathic Palindromic Peptides. |
| AID1411641 | Fungicidal activity against Aspergillus niger ATCC 6275 incubated for 72 hrs followed by serial sub-cultivation for 72 hrs and measured after 72 hrs by serial dilution method | |||
| AID1529081 | Cytotoxicity against lentiviral pLVX-TRE3G-ZsGreen1-CYP3A5 transduced wild type human AsPC1 cells overexpressing CYP3A5 assessed as cell growth | 2020 | Journal of medicinal chemistry, 02-13, Volume: 63, Issue:3 | Clobetasol Propionate Is a Heme-Mediated Selective Inhibitor of Human Cytochrome P450 3A5. |
| AID1387803 | Inhibition of recombinant human CYP3A4 using Luciferin-BE as substrate in presence of NADPH by P450-Glo luminescence assay | |||
| AID1546156 | Antimicrobial activity against Staphylococcus aureus assessed as zone of inhibition at 10 ug/ml | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | Current scenario of tetrazole hybrids for antibacterial activity. |
| AID1574942 | Inhibition of CYP2C19 in human liver microsomes assessed as residual activity at 10 uM using S-mephenytoin as substrate preincubated for 5 mins followed by NADPH addition and measured after 15 mins by LC-MS/MS analysis relative to control | 2019 | Bioorganic & medicinal chemistry letters, 02-01, Volume: 29, Issue:3 | Click chemistry for improvement in selectivity of quinazoline-based kinase inhibitors for mutant epidermal growth factor receptors. |
| AID1399510 | Fungicidal activity against Aspergillus versicolor ATCC 11730 after 144 hrs by serial dilution assay | 2018 | Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16 | 5-Adamantan thiadiazole-based thiazolidinones as antimicrobial agents. Design, synthesis, molecular docking and evaluation. |
| AID1729783 | Fungicidal activity against Candida albicans ATCC 10231 assessed as reduction in fungal load at 125 ug/ml incubated for 48 hrs followed by inoculation on SD agar plate for 48 hrs by time-kill assay | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Design, synthesis, and biodistribution studies of new analogues of marine alkaloids: Potent in vitro and in vivo fungicidal agents against Candida spp. |
| AID1561735 | Inhibition of CYP3A4 in human liver microsomes using midazolam substrate incubated for 10 mins in presence of NADPH | |||
| AID1596697 | Fungicidal activity against Penicillium funiculosum ATCC 36839 incubated for 72 hrs followed by sub-culturing on broth malt medium and measured after 72 hrs | 2019 | European journal of medicinal chemistry, Aug-01, Volume: 175 | Appendix A. dithioloquinolinethiones as new potential multitargeted antibacterial and antifungal agents: Synthesis, biological evaluation and molecular docking studies. |
| AID1412949 | Fungicidal activity against Penicillium ochrochloron ATCC 9112 by microdilution method | 2018 | MedChemComm, May-01, Volume: 9, Issue:5 | Design, synthesis and antimicrobial activity of usnic acid derivatives. |
| AID1721038 | Inhibition of CYP3A4 in human liver microsomes after 20 mins by LC-MS/MS analysis | 2020 | Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17 | Discovery of a Conformationally Constrained Oxazolidinone with Improved Safety and Efficacy Profiles for the Treatment of Multidrug-Resistant Tuberculosis. |
| AID1411639 | Fungicidal activity against Aspergillus ochraceus ATCC 12066 incubated for 72 hrs followed by serial sub-cultivation for 72 hrs and measured after 72 hrs by serial dilution method | |||
| AID1729753 | Antifungal activity against Candida albicans isolate 6 assessed as reduction in fungal growth incubated for 48 hrs by broth microdilution method | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Design, synthesis, and biodistribution studies of new analogues of marine alkaloids: Potent in vitro and in vivo fungicidal agents against Candida spp. |
| AID1652096 | Antifungal activity against Pestalotia calabae assessed as reduction in microbial growth | 2020 | Journal of natural products, 04-24, Volume: 83, Issue:4 | Microketides A and B, Polyketides from a Gorgonian-Derived |
| AID1484680 | Antileishmanial activity against Leishmania braziliensis MHOM/BR/75/M2903 promastigotes forms in presence of terbinafine by trypan blue-staining based light microscopy | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | An overview of azoles targeting sterol 14α-demethylase for antileishmanial therapy. |
| AID1402208 | Antifungal activity against Penicillium chrysogenum assessed as zone of inhibition at 75 ug/well after 48 hrs by agar well diffusion method | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Green approach for the synthesis of thiophenyl pyrazoles and isoxazoles by adopting 1,3-dipolar cycloaddition methodology and their antimicrobial activity. |
| AID1412937 | Antifungal activity against Aspergillus ochraceus by microdilution method | 2018 | MedChemComm, May-01, Volume: 9, Issue:5 | Design, synthesis and antimicrobial activity of usnic acid derivatives. |
| AID1729799 | Antifungal activity against Candida albicans ATCC 10231 assessed as inhibition of yeast to hypha morphological transition at 125 ug/ml measured upto 72 hrs by microscopic analysis | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Design, synthesis, and biodistribution studies of new analogues of marine alkaloids: Potent in vitro and in vivo fungicidal agents against Candida spp. |
| AID1721989 | Fungicidal activity Aspergillus fumigatus | 2020 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 30, Issue:17 | New vinyl-1,2,4-triazole derivatives as antimicrobial agents: Synthesis, biological evaluation and molecular docking studies. |
| AID1739437 | Inhibition of CYP3A4 in human liver microsomes using midazolam as substrate incubated for 5 mins followed by NADPH addition and measured after 20 mins by LC-MS/MS analysis | 2020 | European journal of medicinal chemistry, Aug-15, Volume: 200 | Substituted benzothiophene and benzofuran derivatives as a novel class of bone morphogenetic Protein-2 upregulators: Synthesis, anti-osteoporosis efficacies in ovariectomized rats and a zebrafish model, and ADME properties. |
| AID1529099 | Binding affinity to His-tagged CYP3A4 (unknown origin) expressed in Escherichia coli DH5alpha assessed as induction of new LS formation by EPR spectroscopy | 2020 | Journal of medicinal chemistry, 02-13, Volume: 63, Issue:3 | Clobetasol Propionate Is a Heme-Mediated Selective Inhibitor of Human Cytochrome P450 3A5. |
| AID1411646 | Fungicidal activity against Penicillium ochrochloron ATCC 9112 incubated for 72 hrs followed by serial sub-cultivation for 72 hrs and measured after 72 hrs by serial dilution method | |||
| AID1873201 | Inhibition of human ABCG2 expressed in human HEK293 cells mediated pheophorbide A efflux and measured after 90 mins by FACSflow cytometry | 2022 | European journal of medicinal chemistry, Jul-05, Volume: 237 | Targeting breast cancer resistance protein (BCRP/ABCG2): Functional inhibitors and expression modulators. |
| AID1578466 | Drug concentration in total liver in Wistar Han rat at 1 to 2 mg/kg, iv infused for 10 to 20 hrs by LC-MS/MS analysis | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Structural attributes influencing unbound tissue distribution. |
| AID1614014 | Inhibition of human CYP3A4 in presence of NADPH by luciferase reporter gene assay | 2019 | Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3 | Design, Synthesis, and Biological Evaluation of New 1-(Aryl-1 H-pyrrolyl)(phenyl)methyl-1 H-imidazole Derivatives as Antiprotozoal Agents. |
| AID1729773 | Fungicidal activity against Candida albicans isolate 8 assessed as fungal killing incubated for 48 hrs followed by plating on SD agar plate | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Design, synthesis, and biodistribution studies of new analogues of marine alkaloids: Potent in vitro and in vivo fungicidal agents against Candida spp. |
| AID1721996 | Fungicidal activity Penicillium verrucosum var. cyclopium | 2020 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 30, Issue:17 | New vinyl-1,2,4-triazole derivatives as antimicrobial agents: Synthesis, biological evaluation and molecular docking studies. |
| AID1578474 | Apparent permeability of the compound across dog RRCK cells by MDCK-LE assay | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Structural attributes influencing unbound tissue distribution. |
| AID1833383 | Inhibition of human CYP3A4 at 3.3 uM preincubated with compound followed by substrate and NADP addition by fluorescence assay | |||
| AID1701910 | Inhibition of CYP3A4 in human liver microsomes at 10 uM using midazolam as substrate preincubated for 5 mins followed by NADPH addition and measured after 20 mins by LC-MS/MS analysis relative to control | 2016 | Journal of medicinal chemistry, 12-08, Volume: 59, Issue:23 | Novel Tetrahydropyrido[4,3-d]pyrimidines as Potent Inhibitors of Chaperone Heat Shock Protein 90. |
| AID1369466 | Fungicidal activity against Candida tropicalis cgmcc 2.1975 after 96 hrs | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9 | Combating Drug-Resistant Fungi with Novel Imperfectly Amphipathic Palindromic Peptides. |
| AID1864879 | Antifungal activity against Candida krusei ATCC 6258 assessed as fungal growth inhibition measured after 72 hrs by double dilution method | |||
| AID1411617 | Antifungal activity against Penicillium ochrochloron ATCC 9112 after 72 hrs by serial dilution method | |||
| AID1550860 | Inhibition of CYP3A4 in human liver microsomes using midazolam as substrate incubated for 10 mins after substrate addition by HPLC analysis | 2019 | European journal of medicinal chemistry, Jun-01, Volume: 171 | Synthesis and structure-bactericidal activity relationships of non-ketolides: 9-Oxime clarithromycin 11,12-cyclic carbonate featured with three-to eight-atom-length spacers at 3-OH. |
| AID1497274 | Inhibition of recombinant CYP17 (unknown origin) expressed in human AD293 cells using [21-3H]17alpha-hydroxypregnenolone as substrate preincubated for 60 mins followed by substrate addition measured after 4 hrs Topcount method | 2018 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 28, Issue:13 | Design and synthesis of functionalized piperazin-1yl-(E)-stilbenes as inhibitors of 17α-hydroxylase-C17,20-lyase (Cyp17). |
| AID1769164 | Inhibition of CYP2C19 in human liver microsomes assessed as remaining activity at 1 to 10 uM using (S)-mephenytoin as substrate preincubated for 5 mins followed by addition of NADPH generation system for 15 mins by LC-MS/MS analysis | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | Discovery of G Protein-Biased Antagonists against 5-HT |
| AID1529086 | Cytotoxicity against CRISPR/Cas9-mediated CYP3A5 knock-out and lentiviral pLVX-TRE3G-ZsGreen1-CYP3A5 transduced human AsPC1 cells overexpressing CYP3A5 assessed as cell growth | 2020 | Journal of medicinal chemistry, 02-13, Volume: 63, Issue:3 | Clobetasol Propionate Is a Heme-Mediated Selective Inhibitor of Human Cytochrome P450 3A5. |
| AID1350707 | Apparent permeability cross apical to basolateral side in MDCK-MDR1 cells at 5 uM after 90 mins by LC-MS/MS analysis | 2018 | Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14 | Optimization of Isothiazolo[4,3- b]pyridine-Based Inhibitors of Cyclin G Associated Kinase (GAK) with Broad-Spectrum Antiviral Activity. |
| AID1818562 | Inhibition of CYP3A4 in human liver microsomes using IPA as substrate preincubated for 10 mins followed by NADPH generating system addition and measured after 20 mins | 2022 | Journal of medicinal chemistry, 01-13, Volume: 65, Issue:1 | Discovery and Characterization of Potent Dual P-Glycoprotein and CYP3A4 Inhibitors: Design, Synthesis, Cryo-EM Analysis, and Biological Evaluations. |
| AID1402897 | Induction of apoptosis in Candida krusei ATCC 6258 assessed as necrotic cells at antifungal MIC90 after 24 hrs by Annexin V/propidium iodide staining based flow cytometry (Rvb = 0.9%) | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | The synthesis, antifungal and apoptotic effects of triazole-oxadiazoles against Candida species. |
| AID1402209 | Antifungal activity against Penicillium chrysogenum assessed as zone of inhibition at 100 ug/well after 48 hrs by agar well diffusion method | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Green approach for the synthesis of thiophenyl pyrazoles and isoxazoles by adopting 1,3-dipolar cycloaddition methodology and their antimicrobial activity. |
| AID1369480 | Antifungal activity against Candida albicans cgmcc 2.2086 in presence of MgCl2 by broth dilution method | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9 | Combating Drug-Resistant Fungi with Novel Imperfectly Amphipathic Palindromic Peptides. |
| AID1402894 | Induction of apoptosis in Candida krusei ATCC 6258 assessed as live cells at antifungal MIC90 after 24 hrs by Annexin V/propidium iodide staining based flow cytometry (Rvb = 97.3%) | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | The synthesis, antifungal and apoptotic effects of triazole-oxadiazoles against Candida species. |
| AID1578469 | Unbound tissue partition coefficient, ratio of drug level in brain to plasma in Wistar Han rat at 1 to 2 mg/kg, iv infused for 10 to 20 hrs by LC-MS/MS analysis | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Structural attributes influencing unbound tissue distribution. |
| AID1537340 | Antifungal activity against BFusarium oxysporum CICC 41029 after 48 hrs by broth dilution assay | 2019 | Journal of natural products, 02-22, Volume: 82, Issue:2 | Absolute Configuration of Bioactive Azaphilones from the Marine-Derived Fungus Pleosporales sp. CF09-1. |
| AID1546119 | Antimicrobial activity against Bacillus cereus assessed as zone of inhibition at 250 ug/ml | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | Current scenario of tetrazole hybrids for antibacterial activity. |
| AID1369482 | Antifungal activity against Candida albicans cgmcc 2.2086 in presence of ZnCl2 by broth dilution method | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9 | Combating Drug-Resistant Fungi with Novel Imperfectly Amphipathic Palindromic Peptides. |
| AID1729770 | Fungicidal activity against Candida albicans isolate 5 assessed as fungal killing incubated for 48 hrs followed by plating on SD agar plate | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Design, synthesis, and biodistribution studies of new analogues of marine alkaloids: Potent in vitro and in vivo fungicidal agents against Candida spp. |
| AID1585493 | Induction of phospholipidosis in human HepG2 cells assessed as increase in number of cellular lysosomes at 50 uM after 72 hrs by LYSO-ID Red and Hoechst 33342 staining based fluorescence microscopic method | 2018 | Bioorganic & medicinal chemistry, 12-15, Volume: 26, Issue:23-24 | Optimization and preclinical evaluation of novel histamine H |
| AID1369483 | Antifungal activity against Candida albicans cgmcc 2.2086 in presence of FeCl3 by broth dilution method | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9 | Combating Drug-Resistant Fungi with Novel Imperfectly Amphipathic Palindromic Peptides. |
| AID1411640 | Antifungal activity against Aspergillus niger ATCC 6275 after 72 hrs by serial dilution method | |||
| AID1729778 | Fungicidal activity against Candida albicans isolate 13 assessed as fungal killing incubated for 48 hrs followed by plating on SD agar plate | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Design, synthesis, and biodistribution studies of new analogues of marine alkaloids: Potent in vitro and in vivo fungicidal agents against Candida spp. |
| AID1627885 | Antifungal activity against Candida albicans MTCC 227 at 1 mg/disc after 48 hrs at 28 degC by disc diffusion method | 2016 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 26, Issue:17 | Gold catalyzed double condensation reaction: Synthesis, antimicrobial and cytotoxicity of spirooxindole derivatives. |
| AID1369488 | Antifungal activity against Candida albicans cgmcc 2.2086 in presence of 25% human heat-inactivated serum by broth dilution method | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9 | Combating Drug-Resistant Fungi with Novel Imperfectly Amphipathic Palindromic Peptides. |
| AID1571580 | Antimicrobial activity against Candida albicans 855-653 measured after 14 days by two-fold serial dilution method | 2018 | MedChemComm, Dec-01, Volume: 9, Issue:12 | Design, synthesis, and biological activity of novel ammonium salts containing sterically hindered phenolic fragment and phosphoryl group. |
| AID1811059 | Inhibition of human CYP3A4 using testosterone as substrate in presence of NADPH incubated for 15 to 45 mins | 2021 | Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14 | Improving Druggability of Novel Diarylpyrimidine NNRTIs by a Fragment-Based Replacement Strategy: From Biphenyl-DAPYs to Heteroaromatic-Biphenyl-DAPYs. |
| AID1379941 | Antifungal activity against Candida sake clinical isolates assessed as inhibition of microbial growth incubated for 24 hrs by broth microdilution method | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Synthesis, biological evaluation and quantitative structure-active relationships of 1,3-thiazolidin-4-one derivatives. A promising chemical scaffold endowed with high antifungal potency and low cytotoxicity. |
| AID1412943 | Fungicidal activity against Trichoderma viride IAM 5061 by microdilution method | 2018 | MedChemComm, May-01, Volume: 9, Issue:5 | Design, synthesis and antimicrobial activity of usnic acid derivatives. |
| AID1402214 | Antifungal activity against Aspergillus niger after 48 hrs by broth dilution test | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Green approach for the synthesis of thiophenyl pyrazoles and isoxazoles by adopting 1,3-dipolar cycloaddition methodology and their antimicrobial activity. |
| AID1578470 | Unbound tissue partition coefficient, ratio of drug level in adipose to plasma in Wistar Han rat at 1 to 2 mg/kg, iv infused for 10 to 20 hrs by LC-MS/MS analysis | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Structural attributes influencing unbound tissue distribution. |
| AID1412944 | Fungicidal activity against Aspergillus niger by microdilution method | 2018 | MedChemComm, May-01, Volume: 9, Issue:5 | Design, synthesis and antimicrobial activity of usnic acid derivatives. |
| AID1402204 | Antifungal activity against Aspergillus niger assessed as zone of inhibition at 50 ug/well after 48 hrs by agar well diffusion method | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Green approach for the synthesis of thiophenyl pyrazoles and isoxazoles by adopting 1,3-dipolar cycloaddition methodology and their antimicrobial activity. |
| AID1388193 | Antifungal activity against Trichoderma reesei ATCC 13631 incubated for 24 hrs by serial dilution method | 2017 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 27, Issue:18 | Synthesis, antimicrobial activity, structure-activity relationship and cytotoxic studies of a new series of functionalized (Z)-3-(2-oxo-2-substituted ethylidene)-3,4-dihydro-2H-benzo[b][1,4]oxazin-2-ones. |
| AID1369460 | Fungicidal activity against Candida albicans SP3876 after 96 hrs | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9 | Combating Drug-Resistant Fungi with Novel Imperfectly Amphipathic Palindromic Peptides. |
| AID1656770 | Induction of human HMGCR-dCat-ELuc degradation expressed in HEK293 cells assessed as reduction in luciferase activity measured after 8 hrs in presence of SQS inhibitor TAK-475 by luciferase reporter assay | 2020 | Bioorganic & medicinal chemistry, 02-01, Volume: 28, Issue:3 | Luciferase-based HMG-CoA reductase degradation assay for activity and selectivity profiling of oxy(lano)sterols. |
| AID1595234 | Antifungal activity against Absidia corymbifera assessed as reduction in fungal cell viability by broth dilution method | 2019 | European journal of medicinal chemistry, Jun-01, Volume: 171 | Insights into the chemistry and therapeutic potential of furanones: A versatile pharmacophore. |
| AID1387842 | Inhibition of recombinant human CYP3A4 using Luciferin-BE as substrate at 10 uM in presence of NADPH by P450-Glo luminescence assay relative to control | |||
| AID1595105 | Antifungal activity against Candida albicans NCCS 3471 assessed as inhibition zone at 50 ug/ml by disk diffusion method | 2019 | European journal of medicinal chemistry, May-15, Volume: 170 | Tetrazole hybrids and their antifungal activities. |
| AID1537339 | Antifungal activity against Botryosphaeria dothidea CICC 2678 after 48 hrs by broth dilution assay | 2019 | Journal of natural products, 02-22, Volume: 82, Issue:2 | Absolute Configuration of Bioactive Azaphilones from the Marine-Derived Fungus Pleosporales sp. CF09-1. |
| AID1369534 | Fungicidal activity against Candida albicans 58288 after 96 hrs | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9 | Combating Drug-Resistant Fungi with Novel Imperfectly Amphipathic Palindromic Peptides. |
| AID1702315 | Inhibition of human recombinant CYP3A4 | |||
| AID1721995 | Fungicidal activity Penicillium ochrochloron | 2020 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 30, Issue:17 | New vinyl-1,2,4-triazole derivatives as antimicrobial agents: Synthesis, biological evaluation and molecular docking studies. |
| AID1583039 | Inhibition of CYP3A4 in human liver microsomes using midazolam substrate in presence of NADPH incubated for 10 mins | 2020 | Journal of medicinal chemistry, 02-13, Volume: 63, Issue:3 | Discovery and Characterization of Fluorine-Substituted Diarylpyrimidine Derivatives as Novel HIV-1 NNRTIs with Highly Improved Resistance Profiles and Low Activity for the hERG Ion Channel. |
| AID1764882 | Inhibition of CYP2D6 (unknown origin) assessed as enzyme residual activity at 10 uM | 2021 | European journal of medicinal chemistry, Jun-05, Volume: 218 | Discovery of novel potent migrastatic Thiazolo[5,4-b]pyridines targeting Lysyl-tRNA synthetase (KRS) for treatment of Cancer metastasis. |
| AID1862950 | Inhibition of CYP3A2-mediated metabolite formation in rat liver microsomes assessed as reduction in N-(1-((2R,4R,5R)-3,3-difluoro-4-hydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)-2-oxo-1,2-dihydropyrimidin-4-yl)pentadecanamide metabolism | 2022 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 72 | Design, synthesis and antitumor activity study of a gemcitabine prodrug conjugated with a HDAC6 inhibitor. |
| AID1411638 | Antifungal activity against Aspergillus ochraceus ATCC 12066 after 72 hrs by serial dilution method | |||
| AID1864894 | Antifungal activity against fluconazole -resistant Candida albicans 901 assessed as fungal growth inhibition measured after 72 hrs by double dilution method | |||
| AID1769132 | Inhibition of CYP3A4 in human liver microsomes assessed as remaining activity at 1 to 10 uM using midazolam as substrate preincubated for 5 mins followed by addition of NADPH generation system for 15 mins by LC-MS/MS analysis | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | Discovery of G Protein-Biased Antagonists against 5-HT |
| AID1596692 | Antifungal activity against Trichoderma viride IAM 5061 after 72 hrs by microdilution technique | 2019 | European journal of medicinal chemistry, Aug-01, Volume: 175 | Appendix A. dithioloquinolinethiones as new potential multitargeted antibacterial and antifungal agents: Synthesis, biological evaluation and molecular docking studies. |
| AID1484678 | Antileishmanial activity against Leishmania tropica amastigote forms infected in human monocyte-derived macrophage assessed as reduction in parasite infection at 15 ug/ml relative to control | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | An overview of azoles targeting sterol 14α-demethylase for antileishmanial therapy. |
| AID1402896 | Induction of apoptosis in Candida krusei ATCC 6258 assessed as late apoptotic cells at antifungal MIC90 after 24 hrs by Annexin V/propidium iodide staining based flow cytometry (Rvb = 1.4%) | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | The synthesis, antifungal and apoptotic effects of triazole-oxadiazoles against Candida species. |
| AID1911192 | Inhibition of CYP3A4 in human liver microsomes using midazolam and testosterone as substrate incubated for 5 to 45 mins in presence of NADPH by LC/MS analysis | |||
| AID1402893 | Induction of apoptosis in Candida glabrata ATCC 90030 assessed as necrotic cells at antifungal MIC90 after 24 hrs by Annexin V/propidium iodide staining based flow cytometry (Rvb = 0.3%) | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | The synthesis, antifungal and apoptotic effects of triazole-oxadiazoles against Candida species. |
| AID1484679 | Antileishmanial activity against Leishmania mexicana Walter Reed 227 promastigote forms assessed as reduction in promastigotes sterol biosynthesis at 10 nM after 24 hrs in presence of [2-14C]mevalonate by liquid scintillation spectrometry analysis relativ | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | An overview of azoles targeting sterol 14α-demethylase for antileishmanial therapy. |
| AID1764878 | Inhibition of CYP1A2 (unknown origin) assessed as enzyme residual activity at 10 uM | 2021 | European journal of medicinal chemistry, Jun-05, Volume: 218 | Discovery of novel potent migrastatic Thiazolo[5,4-b]pyridines targeting Lysyl-tRNA synthetase (KRS) for treatment of Cancer metastasis. |
| AID1634151 | Partition coefficient, log P of the compound | 2019 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16 | Strategies for the development of highly selective cytochrome P450 inhibitors: Several CYP targets in current research. |
| AID1617370 | Inhibition of recombinant human CYP3A4 expressed in supersomes using 7-benzyloxyquinoline as substrate by fluorescence method | 2019 | Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22 | Development of Robust 17( |
| AID1520027 | Inhibition of human CYP3A4 preincubated for 5 mins followed by NADPH addition and measured after 30 mins by luminescence based microplate reader analysis | |||
| AID1656498 | Antifungal activity against Candida glabrata assessed as fungal growth inhibition | 2020 | Bioorganic & medicinal chemistry letters, 02-01, Volume: 30, Issue:3 | Design, synthesis and bio-evaluation of C-1 alkylated tetrahydro-β-carboline derivatives as novel antifungal lead compounds. |
| AID1864878 | Antifungal activity against fluconazole- resistant Candida albicans 17# assessed as fungal growth inhibition measured after 72 hrs by double dilution method | |||
| AID1636498 | Drug activation in human Hep3B cells assessed as human CYP2C9-mediated drug metabolism-induced cytotoxicity measured as decrease in cell viability at 34 uM pre-incubated with BSO for 18 hrs followed by incubation with compound for 3 hrs in presence of NAD | 2016 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16 | Development of a cell viability assay to assess drug metabolite structure-toxicity relationships. |
| AID1497276 | Inhibition of human CYP3A4 using testosterone as substrate by LC-MS/MS analysis | 2018 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 28, Issue:13 | Design and synthesis of functionalized piperazin-1yl-(E)-stilbenes as inhibitors of 17α-hydroxylase-C17,20-lyase (Cyp17). |
| AID1872789 | Antifungal activity against Cochliobolus lunatus assessed as zone of inhibition | 2022 | European journal of medicinal chemistry, Apr-15, Volume: 234 | Recent applications of vinyl sulfone motif in drug design and discovery. |
| AID1578458 | Fraction unbound in Wistar Han rat brain at 2 uM incubated for 6 hrs by equilibrium dialysis method | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Structural attributes influencing unbound tissue distribution. |
| AID1683962 | Inhibition of CYP3A4 in in human liver microsomes at 30 uM incubated for 10 mins in presence of CYP3A4 substrate/NADP+ by fluorescence based assay | |||
| AID1403687 | Antifungal activity against Aspergillus niger after 48 hrs by turbidity-based broth dilution assay | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Synthesis and antimicrobial activity of pyrimidinyl 1,3,4-oxadiazoles, 1,3,4-thiadiazoles and 1,2,4-triazoles. |
| AID1497279 | Half-life in guinea pig liver microsomes in presence of NADPH regenerating system by LC/MS/MS method | 2018 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 28, Issue:13 | Design and synthesis of functionalized piperazin-1yl-(E)-stilbenes as inhibitors of 17α-hydroxylase-C17,20-lyase (Cyp17). |
| AID1614063 | Inhibition of recombinant human CYP3A4 using 7-benzyloxy-trifluoromethylcoumarin as substrate preincubated for 10 mins followed by substrate addition and measured after 30 mins | 2019 | Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3 | Evaluation of Amides, Carbamates, Sulfonamides, and Ureas of 4-Prop-2-ynylidenecycloalkylamine as Potent, Selective, and Bioavailable Negative Allosteric Modulators of Metabotropic Glutamate Receptor 5. |
| AID1402886 | Induction of apoptosis in Candida albicans ATCC 90028 assessed as live cells at antifungal MIC90 after 24 hrs by Annexin V/propidium iodide staining based flow cytometry (Rvb = 99.8%) | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | The synthesis, antifungal and apoptotic effects of triazole-oxadiazoles against Candida species. |
| AID1365624 | Antileishmanial activity against Leishmania amazonensis amastigotes assessed as reduction in bacterial lode in early log phase after 24 hrs | 2017 | Bioorganic & medicinal chemistry, 11-01, Volume: 25, Issue:21 | Recently reported biological activities of pyrazole compounds. |
| AID1676228 | Inhibition of CYP3A4 in human liver microsome using midazolam as substrate measured after 20 mins in presence of NADPH by LC-MS/MS analysis | 2020 | Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19 | Novel Human Urate Transporter 1 Inhibitors as Hypouricemic Drug Candidates with Favorable Druggability. |
| AID1484690 | Antileishmanial activity against Leishmania donovani MHOM/N/1983/AG83 promastigote forms after 8 days | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | An overview of azoles targeting sterol 14α-demethylase for antileishmanial therapy. |
| AID1898240 | Inhibition of CYP3A4 in human liver microsomes using midazolam as substrate in presence of NADPH | |||
| AID1529094 | Binding affinity to His-tagged CYP3A4 (unknown origin) expressed in Escherichia coli DH5alpha assessed as type 2 spectral shift by measuring dissociation constant by UV-vis spectrophotometric titration analysis | 2020 | Journal of medicinal chemistry, 02-13, Volume: 63, Issue:3 | Clobetasol Propionate Is a Heme-Mediated Selective Inhibitor of Human Cytochrome P450 3A5. |
| AID1882213 | Antifungal activity against Colletotrichum gloeosporioides | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Natural and synthetic β-carboline as a privileged antifungal scaffolds. |
| AID1822291 | Inhibition of CYP3A4T in human liver microsomes using testosterone as substrate incubated for 15 to 45 mins in presence of NADPH | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 | Discovery of Novel Pyridine-Dimethyl-Phenyl-DAPY Hybrids by Molecular Fusing of Methyl-Pyrimidine-DAPYs and Difluoro-Pyridinyl-DAPYs: Improving the Druggability toward High Inhibitory Activity, Solubility, Safety, and PK. |
| AID1328454 | Selectivity ratio of IC50 for human Cyp3A4 to IC50 for recombinant CYP17 (unknown origin) overexpressed in human AD293 cells | 2016 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 26, Issue:23 | Design, synthesis, and evaluation of (2S,4R)-Ketoconazole sulfonamide analogs as potential treatments for Metabolic Syndrome. |
| AID1776977 | Inhibition of aromatase (unknown origin) | 2021 | Journal of natural products, 06-25, Volume: 84, Issue:6 | Diterpenoids with Aromatase Inhibitory Activity from the Rhizomes of |
| AID1497277 | Selectivity index, ratio of IC50 for human CYP3A4 to IC50 for recombinant CYP17 (unknown origin) | 2018 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 28, Issue:13 | Design and synthesis of functionalized piperazin-1yl-(E)-stilbenes as inhibitors of 17α-hydroxylase-C17,20-lyase (Cyp17). |
| AID1529064 | Inhibition of human recombinant CYP3A5 expressed in supersomes assessed as decrease in formation of D-luciferin at 1.89 uM using luciferin-IPA as substrate incubated for 10 mins in presence of NADPH by P450-Glo luminescence assay relative to control | 2020 | Journal of medicinal chemistry, 02-13, Volume: 63, Issue:3 | Clobetasol Propionate Is a Heme-Mediated Selective Inhibitor of Human Cytochrome P450 3A5. |
| AID1369457 | Fungicidal activity against Candida albicans SP3931 after 96 hrs | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9 | Combating Drug-Resistant Fungi with Novel Imperfectly Amphipathic Palindromic Peptides. |
| AID1662936 | Antifungal activity against Candida pseudotropicalis assessed as fungal growth inhibition by micro-dilution method | 2020 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 30, Issue:13 | Design, synthesis and evaluation of hydrazine and acyl hydrazone derivatives of 5-pyrrolidin-2-one as antifungal agents. |
| AID1769133 | Inhibition of CYP2D6 in human liver microsomes assessed as remaining activity at 1 to 10 uM using dextromethorphan as substrate preincubated for 5 mins followed by addition of NADPH generation system for 15 mins by LC-MS/MS analysis | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | Discovery of G Protein-Biased Antagonists against 5-HT |
| AID1549400 | Inhibition of CYP3A4 in human liver microsomes assessed as reduction in metabolite formation using midazolam as substrate incubated for 10 mins in presence of NADPH by HPLC based mass spectrometric method | 2019 | European journal of medicinal chemistry, May-01, Volume: 169 | Design, synthesis and structure-activity relationships of novel macrolones: Hybrids of 2-fluoro 9-oxime ketolides and carbamoyl quinolones with highly improved activity against resistant pathogens. |
| AID1508088 | Antifungal activity against Aspergillus niger | 2017 | European journal of medicinal chemistry, Sep-29, Volume: 138 | Azaphenothiazines - promising phenothiazine derivatives. An insight into nomenclature, synthesis, structure elucidation and biological properties. |
| AID1729765 | Fungicidal activity against Candida tropicalis ATCC 28707 assessed as fungal killing incubated for 48 hrs followed by plating on SD agar plate | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Design, synthesis, and biodistribution studies of new analogues of marine alkaloids: Potent in vitro and in vivo fungicidal agents against Candida spp. |
| AID1546121 | Antimicrobial activity against Pseudomonas aeruginosa assessed as zone of inhibition at 250 ug/ml | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | Current scenario of tetrazole hybrids for antibacterial activity. |
| AID1402895 | Induction of apoptosis in Candida krusei ATCC 6258 assessed as early apoptotic cells at antifungal MIC90 after 24 hrs by Annexin V/propidium iodide staining based flow cytometry (Rvb = 0.5%) | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | The synthesis, antifungal and apoptotic effects of triazole-oxadiazoles against Candida species. |
| AID1882559 | Inhibition of recombinant Trypanosoma cruzi Tulahuen strain CYP51 expressed in Escherichia coli JM109 | 2022 | Bioorganic & medicinal chemistry, 03-15, Volume: 58 | Examination of multiple Trypanosoma cruzi targets in a new drug discovery approach for Chagas disease. |
| AID1662853 | Fungicidal activity against Candida albicans | 2020 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 30, Issue:13 | Design and synthesis of amphiphilic 2-hydroxybenzylphosphonium salts with antimicrobial and antitumor dual action. |
| AID1729776 | Fungicidal activity against Candida albicans isolate 11 assessed as fungal killing incubated for 48 hrs followed by plating on SD agar plate | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Design, synthesis, and biodistribution studies of new analogues of marine alkaloids: Potent in vitro and in vivo fungicidal agents against Candida spp. |
| AID1529087 | Cytotoxicity against CRISPR/Cas9-mediated CYP3A5 knock-out and doxycycline-induced CYP3A5 overexpressing human AsPC1 cells assessed as cell growth | 2020 | Journal of medicinal chemistry, 02-13, Volume: 63, Issue:3 | Clobetasol Propionate Is a Heme-Mediated Selective Inhibitor of Human Cytochrome P450 3A5. |
| AID1402215 | Antifungal activity against Penicillium chrysogenum after 48 hrs by broth dilution test | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Green approach for the synthesis of thiophenyl pyrazoles and isoxazoles by adopting 1,3-dipolar cycloaddition methodology and their antimicrobial activity. |
| AID1652094 | Antifungal activity against Colletotrichum truncatum assessed as reduction in microbial growth | 2020 | Journal of natural products, 04-24, Volume: 83, Issue:4 | Microketides A and B, Polyketides from a Gorgonian-Derived |
| AID1412939 | Antifungal activity against Trichoderma viride IAM 5061 by microdilution method | 2018 | MedChemComm, May-01, Volume: 9, Issue:5 | Design, synthesis and antimicrobial activity of usnic acid derivatives. |
| AID1729757 | Antifungal activity against Candida albicans isolate 10 assessed as reduction in fungal growth incubated for 48 hrs by broth microdilution method | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Design, synthesis, and biodistribution studies of new analogues of marine alkaloids: Potent in vitro and in vivo fungicidal agents against Candida spp. |
| AID1863230 | Inhibition of CYP3A4 in human liver microsomes using midazolam as substrate and measured by LC-MS/MS analysis | 2022 | European journal of medicinal chemistry, Oct-05, Volume: 240 | 4th generation nonsteroidal aromatase inhibitors: An iterative SAR-guided design, synthesis, and biological evaluation towards picomolar dual binding inhibitors. |
| AID1403682 | Antifungal activity against Penicillium chrysogenum assessed as diameter of inhibition zone at 100 ug/well after 48 hrs by agar well diffusion method | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Synthesis and antimicrobial activity of pyrimidinyl 1,3,4-oxadiazoles, 1,3,4-thiadiazoles and 1,2,4-triazoles. |
| AID1769163 | Inhibition of CYP2C9 in human liver microsomes assessed as remaining activity at 1 to 10 uM using diclofenac as substrate preincubated for 5 mins followed by addition of NADPH generation system for 15 mins by LC-MS/MS analysis | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | Discovery of G Protein-Biased Antagonists against 5-HT |
| AID1729767 | Fungicidal activity against Candida albicans isolate 2 assessed as fungal killing incubated for 48 hrs followed by plating on SD agar plate | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Design, synthesis, and biodistribution studies of new analogues of marine alkaloids: Potent in vitro and in vivo fungicidal agents against Candida spp. |
| AID1813641 | Inhibition of CYP3A4 in human liver microsome using testosterone as substrate | 2021 | Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23 | Synthesis, Characterization, and Preclinical Evaluation of a Small-Molecule Prostate-Specific Membrane Antigen-Targeted Monomethyl Auristatin E Conjugate. |
| AID1379936 | Antifungal activity against Candida albicans clinical isolates assessed as inhibition of microbial growth incubated for 24 hrs by broth microdilution method | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Synthesis, biological evaluation and quantitative structure-active relationships of 1,3-thiazolidin-4-one derivatives. A promising chemical scaffold endowed with high antifungal potency and low cytotoxicity. |
| AID1529084 | Cytotoxicity against CRISPR/Cas9-mediated CYP3A5 knock-out human AsPC1 cells assessed as cell growth | 2020 | Journal of medicinal chemistry, 02-13, Volume: 63, Issue:3 | Clobetasol Propionate Is a Heme-Mediated Selective Inhibitor of Human Cytochrome P450 3A5. |
| AID1729759 | Antifungal activity against Candida albicans isolate 12 assessed as reduction in fungal growth incubated for 48 hrs by broth microdilution method | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Design, synthesis, and biodistribution studies of new analogues of marine alkaloids: Potent in vitro and in vivo fungicidal agents against Candida spp. |
| AID1674183 | Inhibition of human BSEP expressed in HEK293 cell membrane vesicles assessed as reduction in 3H-TCA uptake incubated for 5 mins by radiodetection method | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20 | Drug Induced Liver Injury (DILI). Mechanisms and Medicinal Chemistry Avoidance/Mitigation Strategies. |
| AID1369450 | Antifungal activity against fluconazole-resistant Candida albicans 56214 after 48 hrs by broth microdilution method | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9 | Combating Drug-Resistant Fungi with Novel Imperfectly Amphipathic Palindromic Peptides. |
| AID1351507 | Inhibition of CYP3A4 (unknown origin) after 2 hrs by firefly luciferase-luminescence based P450-glo assay | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Novel non-sulfonamide 5-HT |
| AID1350727 | Aqueous solubility in PBS buffer at pH 7.4 at 100 uM after 1 hr by LC-MS/MS analysis | 2018 | Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14 | Optimization of Isothiazolo[4,3- b]pyridine-Based Inhibitors of Cyclin G Associated Kinase (GAK) with Broad-Spectrum Antiviral Activity. |
| AID1403675 | Antifungal activity against Aspergillus niger assessed as diameter of inhibition zone at 12.5 ug/well after 48 hrs by agar well diffusion method | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Synthesis and antimicrobial activity of pyrimidinyl 1,3,4-oxadiazoles, 1,3,4-thiadiazoles and 1,2,4-triazoles. |
| AID1771187 | Inhibition of CYP3A4 (unknown origin) assessed as activity using midazolam as substrate at 0.003 uM relative to control | 2021 | Journal of medicinal chemistry, 09-09, Volume: 64, Issue:17 | Discovery of |
| AID1388198 | Antifungal activity against Fusarium oxysporum ATCC 62506 at 100 ug/ml incubated for 72 hrs by agar disc diffusion assay | 2017 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 27, Issue:18 | Synthesis, antimicrobial activity, structure-activity relationship and cytotoxic studies of a new series of functionalized (Z)-3-(2-oxo-2-substituted ethylidene)-3,4-dihydro-2H-benzo[b][1,4]oxazin-2-ones. |
| AID1402206 | Antifungal activity against Aspergillus niger assessed as zone of inhibition at 100 ug/well after 48 hrs by agar well diffusion method | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Green approach for the synthesis of thiophenyl pyrazoles and isoxazoles by adopting 1,3-dipolar cycloaddition methodology and their antimicrobial activity. |
| AID1412947 | Fungicidal activity against Aspergillus fumigatus ATCC 1022 by microdilution method | 2018 | MedChemComm, May-01, Volume: 9, Issue:5 | Design, synthesis and antimicrobial activity of usnic acid derivatives. |
| AID1369468 | Fungicidal activity against Candida parapsilosis cgmcc 2.3989 after 96 hrs | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9 | Combating Drug-Resistant Fungi with Novel Imperfectly Amphipathic Palindromic Peptides. |
| AID1574938 | Inhibition of CYP2A6 in human liver microsomes assessed as residual activity at 10 uM using coumarin as substrate preincubated for 5 mins followed by NADPH addition and measured after 15 mins by LC-MS/MS analysis relative to control | 2019 | Bioorganic & medicinal chemistry letters, 02-01, Volume: 29, Issue:3 | Click chemistry for improvement in selectivity of quinazoline-based kinase inhibitors for mutant epidermal growth factor receptors. |
| AID1402898 | Induction of apoptosis in Candida parapsilosis ATCC 22019 assessed as live cells at antifungal MIC90 after 24 hrs by Annexin V/propidium iodide staining based flow cytometry (Rvb = 97.6%) | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | The synthesis, antifungal and apoptotic effects of triazole-oxadiazoles against Candida species. |
| AID1388200 | Antifungal activity against Penicillium funiculosum ATCC 11797 at 100 ug/ml incubated for 72 hrs by agar disc diffusion assay | 2017 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 27, Issue:18 | Synthesis, antimicrobial activity, structure-activity relationship and cytotoxic studies of a new series of functionalized (Z)-3-(2-oxo-2-substituted ethylidene)-3,4-dihydro-2H-benzo[b][1,4]oxazin-2-ones. |
| AID1529079 | Increase in CYP3A4 expression in CRISPR/Cas9-mediated CYP3A5 knock-out and doxycycline-induced CYP3A4 overexpressing human AsPC1 cells at 1 uM after 24 hrs by Western blot analysis | 2020 | Journal of medicinal chemistry, 02-13, Volume: 63, Issue:3 | Clobetasol Propionate Is a Heme-Mediated Selective Inhibitor of Human Cytochrome P450 3A5. |
| AID1572535 | Inhibition of CYP3A4 in human liver microsomes using midazolam as substrate after 3 mins in presence of NADP by LC-MS/MS analysis | |||
| AID1369487 | Antifungal activity against Candida albicans cgmcc 2.2086 in presence of 12.5% human heat-inactivated serum by broth dilution method | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9 | Combating Drug-Resistant Fungi with Novel Imperfectly Amphipathic Palindromic Peptides. |
| AID1411634 | Antifungal activity against Aspergillus versicolor ATCC 11730 after 72 hrs by serial dilution method | |||
| AID1721990 | Fungicidal activity Aspergillus versicolor | 2020 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 30, Issue:17 | New vinyl-1,2,4-triazole derivatives as antimicrobial agents: Synthesis, biological evaluation and molecular docking studies. |
| AID1328449 | Inhibition of recombinant CYP17 (unknown origin) overexpressed in human AD293 cells using [21-3H]17alpha-hydroxyl-pregenolone as substrate preincubated for 60 mins followed by substrate addition measured after 4 hrs by Topcount method | 2016 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 26, Issue:23 | Design, synthesis, and evaluation of (2S,4R)-Ketoconazole sulfonamide analogs as potential treatments for Metabolic Syndrome. |
| AID1388190 | Antifungal activity against Fusarium oxysporum ATCC 62506 incubated for 24 hrs by serial dilution method | 2017 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 27, Issue:18 | Synthesis, antimicrobial activity, structure-activity relationship and cytotoxic studies of a new series of functionalized (Z)-3-(2-oxo-2-substituted ethylidene)-3,4-dihydro-2H-benzo[b][1,4]oxazin-2-ones. |
| AID1365626 | Antileishmanial activity against Leishmania amazonensis axenic amastigotes after 24 hrs | 2017 | Bioorganic & medicinal chemistry, 11-01, Volume: 25, Issue:21 | Recently reported biological activities of pyrazole compounds. |
| AID1882175 | Antifungal activity against Saccharomyces cerevisiae | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Natural and synthetic β-carboline as a privileged antifungal scaffolds. |
| AID1412945 | Fungicidal activity against Aspergillus ochraceus by microdilution method | 2018 | MedChemComm, May-01, Volume: 9, Issue:5 | Design, synthesis and antimicrobial activity of usnic acid derivatives. |
| AID1770976 | Inhibition of CYP3A4 in human liver Microsome using midazolam as substrate preincubated for 10 mins followed by NADPH addition and further incubated for 10 mins as substrate by LC-MS/MS analysis relative to control | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Design, synthesis and evaluation of novel 5-phenylthiophene derivatives as potent fungicidal of Candida albicans and antifungal reagents of fluconazole-resistant fungi. |
| AID1652095 | Antifungal activity against Gloeosporium musarum assessed as reduction in microbial growth | 2020 | Journal of natural products, 04-24, Volume: 83, Issue:4 | Microketides A and B, Polyketides from a Gorgonian-Derived |
| AID1596687 | Fungicidal activity against Aspergillus versicolor ATCC 11730 incubated for 72 hrs followed by sub-culturing on broth malt medium and measured after 72 hrs | 2019 | European journal of medicinal chemistry, Aug-01, Volume: 175 | Appendix A. dithioloquinolinethiones as new potential multitargeted antibacterial and antifungal agents: Synthesis, biological evaluation and molecular docking studies. |
| AID1721987 | Antifungal activity Penicillium ochrochloron by microdilution method | 2020 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 30, Issue:17 | New vinyl-1,2,4-triazole derivatives as antimicrobial agents: Synthesis, biological evaluation and molecular docking studies. |
| AID1407676 | Inhibition of recombinant human CYP3A4 expressed in insect cell microsomes at 5 uM using Luciferin-IPA as substrate preincubated for 10 mins followed by NADPH addition measured after 10 mins by luminometric method | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Hedgehog pathway inhibitors of the acylthiourea and acylguanidine class show antitumor activity on colon cancer in vitro and in vivo. |
| AID1402887 | Induction of apoptosis in Candida albicans ATCC 90028 assessed as early apoptotic cells at antifungal MIC90 after 24 hrs by Annexin V/propidium iodide staining based flow cytometry (Rvb = 0%) | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | The synthesis, antifungal and apoptotic effects of triazole-oxadiazoles against Candida species. |
| AID1721992 | Fungicidal activity Aspergillus niger | 2020 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 30, Issue:17 | New vinyl-1,2,4-triazole derivatives as antimicrobial agents: Synthesis, biological evaluation and molecular docking studies. |
| AID1399220 | Inhibition of CYP3A4 in human liver microsomes at 1 uM using midazolam as substrate by LC-MS/MS analysis relative to control | 2018 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 28, Issue:18 | Design, synthesis and biological evaluation of a series of novel GPR40 agonists containing nitrogen heterocyclic rings. |
| AID1918336 | Antifungal activity against Aspergillus fumigatus KM8001 assessed as inhibition of fungal growth measured after 72 hrs by CLSI based liquid medium dilution method | 2022 | Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21 | Novel Aryl Alkamidazole Derivatives as Multifunctional Antifungal Inhibitors: Design, Synthesis, and Biological Evaluation. |
| AID1658921 | Inhibition of CYP3A4 (unknown origin) expressed in insect cell microsomes using dibenzylfluorescein substrate by fluorescence based assay | 2020 | Journal of medicinal chemistry, 07-23, Volume: 63, Issue:14 | Nitrogen-Walk Approach to Explore Bioisosteric Replacements in a Series of Potent A |
| AID1369479 | Antifungal activity against Candida albicans cgmcc 2.2086 in presence of NH4Cl by broth dilution method | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9 | Combating Drug-Resistant Fungi with Novel Imperfectly Amphipathic Palindromic Peptides. |
| AID1729772 | Fungicidal activity against Candida albicans isolate 7 assessed as fungal killing incubated for 48 hrs followed by plating on SD agar plate | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Design, synthesis, and biodistribution studies of new analogues of marine alkaloids: Potent in vitro and in vivo fungicidal agents against Candida spp. |
| AID1351508 | Inhibition of CYP2D6 (unknown origin) after 2 hrs by firefly luciferase-luminescence based P450-glo assay | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Novel non-sulfonamide 5-HT |
| AID1571587 | Bactericidal activity against Candida albicans 855-653 measured after 4 hrs | 2018 | MedChemComm, Dec-01, Volume: 9, Issue:12 | Design, synthesis, and biological activity of novel ammonium salts containing sterically hindered phenolic fragment and phosphoryl group. |
| AID1411645 | Fungicidal activity against Penicillium funiculosum ATCC 36839 incubated for 72 hrs followed by serial sub-cultivation for 72 hrs and measured after 72 hrs by serial dilution method | |||
| AID1662851 | Fungicidal activity against Trichophyton mentagrophytes | 2020 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 30, Issue:13 | Design and synthesis of amphiphilic 2-hydroxybenzylphosphonium salts with antimicrobial and antitumor dual action. |
| AID1596698 | Antifungal activity against Penicillium verrucosum var. cyclopium food isolate after 72 hrs by microdilution technique | 2019 | European journal of medicinal chemistry, Aug-01, Volume: 175 | Appendix A. dithioloquinolinethiones as new potential multitargeted antibacterial and antifungal agents: Synthesis, biological evaluation and molecular docking studies. |
| AID1578456 | Fraction unbound in Wistar Han rat plasma at 2 uM incubated for 6 hrs by equilibrium dialysis method | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Structural attributes influencing unbound tissue distribution. |
| AID1369455 | Antifungal activity against Candida parapsilosis cgmcc 2.3989 after 48 hrs by broth microdilution method | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9 | Combating Drug-Resistant Fungi with Novel Imperfectly Amphipathic Palindromic Peptides. |
| AID1369477 | Antifungal activity against Candida albicans cgmcc 2.2086 in presence of NaCl by broth dilution method | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9 | Combating Drug-Resistant Fungi with Novel Imperfectly Amphipathic Palindromic Peptides. |
| AID1862035 | Inhibition of rat CYP3A4 in rat liver microsomes assessed as inhibition of midazolam metabolism using midazolam as substrate at 10 uM incubated for 10 mins relative to control | 2022 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 72 | Discovery of benzyloxyphenyl- and phenethylphenyl-imidazole derivatives as a new class of ante-drug type boosters. |
| AID1721983 | Antifungal activity Aspergillus ochraceus by microdilution method | 2020 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 30, Issue:17 | New vinyl-1,2,4-triazole derivatives as antimicrobial agents: Synthesis, biological evaluation and molecular docking studies. |
| AID1918337 | Antifungal activity against fluconazole-resistant Candida albicans 17# assessed as inhibition of fungal growth measured after 72 hrs by CLSI based liquid medium dilution method | 2022 | Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21 | Novel Aryl Alkamidazole Derivatives as Multifunctional Antifungal Inhibitors: Design, Synthesis, and Biological Evaluation. |
| AID1729745 | Antifungal activity against Candida glabrata ATCC 2001 assessed as reduction in fungal growth incubated for 48 hrs by broth microdilution method | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Design, synthesis, and biodistribution studies of new analogues of marine alkaloids: Potent in vitro and in vivo fungicidal agents against Candida spp. |
| AID1369458 | Fungicidal activity against Candida albicans SP3903 after 96 hrs | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9 | Combating Drug-Resistant Fungi with Novel Imperfectly Amphipathic Palindromic Peptides. |
| AID1886462 | Inhibition of CYP3A4 in human liver microsomes incubated for 10 mins in the presence of NADPH by high performance liquid chromatography-tandem mass spectrometry | |||
| AID1578464 | Drug concentration in total brain in Wistar Han rat at 1 to 2 mg/kg, iv infused for 10 to 20 hrs by LC-MS/MS analysis | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Structural attributes influencing unbound tissue distribution. |
| AID1529089 | Binding affinity to heme in His-tagged CYP3A5 (unknown origin) expressed in Escherichia coli DH5alpha assessed as retention of six coordinate ferric heme iron by measuring type 2 Soret shift from 417 nm to 424 nm by UV-vis spectrophotometric titration ana | 2020 | Journal of medicinal chemistry, 02-13, Volume: 63, Issue:3 | Clobetasol Propionate Is a Heme-Mediated Selective Inhibitor of Human Cytochrome P450 3A5. |
| AID1864893 | Antifungal activity against fluconazole -resistant Candida albicans 632 assessed as fungal growth inhibition measured after 72 hrs by double dilution method | |||
| AID1574937 | Inhibition of CYP1A2 in human liver microsomes assessed as residual activity at 10 uM using phenacetin as substrate preincubated for 5 mins followed by NADPH addition and measured after 15 mins by LC-MS/MS analysis relative to control | 2019 | Bioorganic & medicinal chemistry letters, 02-01, Volume: 29, Issue:3 | Click chemistry for improvement in selectivity of quinazoline-based kinase inhibitors for mutant epidermal growth factor receptors. |
| AID1918339 | Antifungal activity against fluconazole-resistant Candida albicans 632 assessed as inhibition of fungal growth measured after 72 hrs by CLSI based liquid medium dilution method | 2022 | Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21 | Novel Aryl Alkamidazole Derivatives as Multifunctional Antifungal Inhibitors: Design, Synthesis, and Biological Evaluation. |
| AID1379938 | Antifungal activity against Candida tropicalis clinical isolates assessed as inhibition of microbial growth incubated for 24 hrs by broth microdilution method | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Synthesis, biological evaluation and quantitative structure-active relationships of 1,3-thiazolidin-4-one derivatives. A promising chemical scaffold endowed with high antifungal potency and low cytotoxicity. |
| AID1403677 | Antifungal activity against Aspergillus niger assessed as diameter of inhibition zone at 50 ug/well after 48 hrs by agar well diffusion method | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Synthesis and antimicrobial activity of pyrimidinyl 1,3,4-oxadiazoles, 1,3,4-thiadiazoles and 1,2,4-triazoles. |
| AID1403681 | Antifungal activity against Penicillium chrysogenum assessed as diameter of inhibition zone at 50 ug/well after 48 hrs by agar well diffusion method | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Synthesis and antimicrobial activity of pyrimidinyl 1,3,4-oxadiazoles, 1,3,4-thiadiazoles and 1,2,4-triazoles. |
| AID1529074 | Inhibition of CYP3A5 in wild type human AsPC1 cells assessed as decrease in 1-hydroxymidazolam formation using midazolam as substrate after 24 hrs by LC-MS/MS analysis | 2020 | Journal of medicinal chemistry, 02-13, Volume: 63, Issue:3 | Clobetasol Propionate Is a Heme-Mediated Selective Inhibitor of Human Cytochrome P450 3A5. |
| AID1546122 | Antifungal activity against Candida albicans assessed as zone of inhibition at 250 ug/ml | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | Current scenario of tetrazole hybrids for antibacterial activity. |
| AID1388191 | Antifungal activity against Aspergillus niger ATCC 9029 incubated for 24 hrs by serial dilution method | 2017 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 27, Issue:18 | Synthesis, antimicrobial activity, structure-activity relationship and cytotoxic studies of a new series of functionalized (Z)-3-(2-oxo-2-substituted ethylidene)-3,4-dihydro-2H-benzo[b][1,4]oxazin-2-ones. |
| AID1874530 | 1-Octanol/phosphate buffer partition coefficient, logD of the compound measured after 4.5 hrs by HPLC-UV analysis | 2022 | Journal of medicinal chemistry, 09-08, Volume: 65, Issue:17 | Development, Optimization, and In Vivo Validation of New Imidazopyridine Chemotypes as Dual TLR7/TLR9 Antagonists through Activity-Directed Sequential Incorporation of Relevant Structural Subunits. |
| AID1729760 | Antifungal activity against Candida albicans isolate 13 assessed as reduction in fungal growth incubated for 48 hrs by broth microdilution method | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Design, synthesis, and biodistribution studies of new analogues of marine alkaloids: Potent in vitro and in vivo fungicidal agents against Candida spp. |
| AID1662937 | Antifungal activity against Candida tropicalis assessed as fungal growth inhibition by micro-dilution method | 2020 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 30, Issue:13 | Design, synthesis and evaluation of hydrazine and acyl hydrazone derivatives of 5-pyrrolidin-2-one as antifungal agents. |
| AID1891098 | Plasma protein binding in human plasma at 10 uM incubated for 6 hrs by LC-MS/MS based equilibrium dialysis method | 2022 | European journal of medicinal chemistry, Jun-05, Volume: 236 | Synthesis and biological evaluation of 1,2,4-triazole derivatives as potential Nrf2 activators for the treatment of cerebral ischemic injury. |
| AID1574939 | Inhibition of CYP2B6 in human liver microsomes assessed as residual activity at 10 uM using bupropion as substrate preincubated for 5 mins followed by NADPH addition and measured after 15 mins by LC-MS/MS analysis relative to control | 2019 | Bioorganic & medicinal chemistry letters, 02-01, Volume: 29, Issue:3 | Click chemistry for improvement in selectivity of quinazoline-based kinase inhibitors for mutant epidermal growth factor receptors. |
| AID1402888 | Induction of apoptosis in Candida albicans ATCC 90028 assessed as late apoptotic cells at antifungal MIC90 after 24 hrs by Annexin V/propidium iodide staining based flow cytometry (Rvb = 0%) | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | The synthesis, antifungal and apoptotic effects of triazole-oxadiazoles against Candida species. |
| AID1537287 | Antifungal activity against Sclerotinia sclerotiorum after 3 to 7 days by microbroth dilution method | 2019 | Journal of natural products, 02-22, Volume: 82, Issue:2 | Prenylated Indole Diterpene Alkaloids from a Mine-Soil-Derived Tolypocladium sp. |
| AID1412946 | Fungicidal activity against Aspergillus versicolor ATCC 11730 by microdilution method | 2018 | MedChemComm, May-01, Volume: 9, Issue:5 | Design, synthesis and antimicrobial activity of usnic acid derivatives. |
| AID1508080 | Antifungal activity against Aspergillus niger by CLSI protocol based method | 2017 | European journal of medicinal chemistry, Sep-29, Volume: 138 | Azaphenothiazines - promising phenothiazine derivatives. An insight into nomenclature, synthesis, structure elucidation and biological properties. |
| AID1713221 | Growth inhibition of androgen-insensitive human PC3 cells incubated for 48 hrs by sulforhodamine B assay | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Synthesis of 17β-N-arylcarbamoylandrost-4-en-3-one derivatives and their anti-proliferative effect on human androgen-sensitive LNCaP cell line. |
| AID1399512 | Fungicidal activity against Aspergillus ochraceus ATCC 12066 after 144 hrs by serial dilution assay | 2018 | Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16 | 5-Adamantan thiadiazole-based thiazolidinones as antimicrobial agents. Design, synthesis, molecular docking and evaluation. |
| AID1729752 | Antifungal activity against Candida albicans isolate 5 assessed as reduction in fungal growth incubated for 48 hrs by broth microdilution method | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Design, synthesis, and biodistribution studies of new analogues of marine alkaloids: Potent in vitro and in vivo fungicidal agents against Candida spp. |
| AID1399518 | Fungicidal activity against Penicillium funiculosum ATCC 36839 after 144 hrs by serial dilution assay | 2018 | Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16 | 5-Adamantan thiadiazole-based thiazolidinones as antimicrobial agents. Design, synthesis, molecular docking and evaluation. |
| AID1729744 | Antifungal activity against Candida albicans ATCC 18804 assessed as reduction in fungal growth incubated for 48 hrs by broth microdilution method | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Design, synthesis, and biodistribution studies of new analogues of marine alkaloids: Potent in vitro and in vivo fungicidal agents against Candida spp. |
| AID1508089 | Antimicrobial activity against Candida albicans | 2017 | European journal of medicinal chemistry, Sep-29, Volume: 138 | Azaphenothiazines - promising phenothiazine derivatives. An insight into nomenclature, synthesis, structure elucidation and biological properties. |
| AID1369467 | Fungicidal activity against Candida krusei cgmcc 2.1857 after 96 hrs | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9 | Combating Drug-Resistant Fungi with Novel Imperfectly Amphipathic Palindromic Peptides. |
| AID1546157 | Antifungal activity against Candida albicans assessed as zone of inhibition at 10 ug/ml | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | Current scenario of tetrazole hybrids for antibacterial activity. |
| AID1729755 | Antifungal activity against Candida albicans isolate 8 assessed as reduction in fungal growth incubated for 48 hrs by broth microdilution method | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Design, synthesis, and biodistribution studies of new analogues of marine alkaloids: Potent in vitro and in vivo fungicidal agents against Candida spp. |
| AID1399517 | Antifungal activity against Penicillium funiculosum ATCC 36839 after 72 hrs by serial dilution assay | 2018 | Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16 | 5-Adamantan thiadiazole-based thiazolidinones as antimicrobial agents. Design, synthesis, molecular docking and evaluation. |
| AID1537281 | Antifungal activity against Alternaria fragaria after 3 to 7 days by microbroth dilution method | 2019 | Journal of natural products, 02-22, Volume: 82, Issue:2 | Prenylated Indole Diterpene Alkaloids from a Mine-Soil-Derived Tolypocladium sp. |
| AID1833888 | Binding affinity to Naegleria fowleri CYP51 expressed in Escherichia coli HMS-174 (DE3) assessed as dissociation constant by quadratic Morrison equation | 2021 | Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23 | Relaxed Substrate Requirements of Sterol 14α-Demethylase from |
| AID1704644 | Inhibition of human CYP24A1 expressed in Chinese hamster V79 cells using [3H-1beta]-1alpha,25(OH)2D3 as substrate preincubated for 10 mins followed by substrate addition and measured after 2 hrs by scintillation counting method | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23 | Sulfoximines as Rising Stars in Modern Drug Discovery? Current Status and Perspective on an Emerging Functional Group in Medicinal Chemistry. |
| AID1402205 | Antifungal activity against Aspergillus niger assessed as zone of inhibition at 75 ug/well after 48 hrs by agar well diffusion method | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Green approach for the synthesis of thiophenyl pyrazoles and isoxazoles by adopting 1,3-dipolar cycloaddition methodology and their antimicrobial activity. |
| AID1347151 | Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID504836 | Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation | 2002 | The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16 | Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells. |
| AID1347083 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1508630 | Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
| AID1347057 | CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation | 2019 | PloS one, , Volume: 14, Issue:7 | Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors. |
| AID588378 | qHTS for Inhibitors of ATXN expression: Validation | |||
| AID1347086 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID588349 | qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay | |||
| AID1347049 | Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen | 2019 | Science translational medicine, 07-10, Volume: 11, Issue:500 | Inhibition of natriuretic peptide receptor 1 reduces itch in mice. |
| AID1347082 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347405 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| AID1347050 | Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay | 2019 | Science translational medicine, 07-10, Volume: 11, Issue:500 | Inhibition of natriuretic peptide receptor 1 reduces itch in mice. |
| AID1347410 | qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library | 2019 | Cellular signalling, 08, Volume: 60 | A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening. |
| AID1347058 | CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation | 2019 | PloS one, , Volume: 14, Issue:7 | Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors. |
| AID504812 | Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
| AID1347059 | CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation | 2019 | PloS one, , Volume: 14, Issue:7 | Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors. |
| AID504810 | Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
| AID1347045 | Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line | 2019 | Science translational medicine, 07-10, Volume: 11, Issue:500 | Inhibition of natriuretic peptide receptor 1 reduces itch in mice. |
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| AID1347092 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347103 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347102 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347089 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347097 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347106 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347094 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347091 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347101 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347104 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347099 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347100 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347105 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347095 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347108 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347098 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347154 | Primary screen GU AMC qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347090 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347107 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347096 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1347093 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
| AID1796205 | CYP11B assay from Article 10.1021/jm0492397: \\Synthesis and evaluation of (pyridylmethylene)tetrahydronaphthalenes/-indanes and structurally modified derivatives: potent and selective inhibitors of aldosterone synthase.\\ | 2005 | Journal of medicinal chemistry, Mar-10, Volume: 48, Issue:5 | Synthesis and evaluation of (pyridylmethylene)tetrahydronaphthalenes/-indanes and structurally modified derivatives: potent and selective inhibitors of aldosterone synthase. |
| AID1799528 | Inhibition Assay from Article 10.1016/j.chembiol.2007.10.011: \\Sterol 14alpha-demethylase as a potential target for antitrypanosomal therapy: enzyme inhibition and parasite cell growth.\\ | 2007 | Chemistry & biology, Nov, Volume: 14, Issue:11 | Sterol 14alpha-demethylase as a potential target for antitrypanosomal therapy: enzyme inhibition and parasite cell growth. |
| AID1799838 | CYP27B1 Inhibition Assay from Article 10.1021/bi101488p: \\Screening of selective inhibitors of 1a,25-dihydroxyvitamin D3 24-hydroxylase using recombinant human enzyme expressed in Escherichia coli.\\ | 2010 | Biochemistry, Dec-14, Volume: 49, Issue:49 | Screening of selective inhibitors of 1α,25-dihydroxyvitamin D3 24-hydroxylase using recombinant human enzyme expressed in Escherichia coli. |
| AID1799791 | Binding Assay from Article 10.1074/jbc.M110.164293: \\Structural and biochemical characterization of Mycobacterium tuberculosis CYP142: evidence for multiple cholesterol 27-hydroxylase activities in a human pathogen.\\ | 2010 | The Journal of biological chemistry, Dec-03, Volume: 285, Issue:49 | Structural and biochemical characterization of Mycobacterium tuberculosis CYP142: evidence for multiple cholesterol 27-hydroxylase activities in a human pathogen. |
| AID1796255 | CYP11B Assay from Article 10.1021/jm060055x: \\Synthesis and evaluation of heteroaryl-substituted dihydronaphthalenes and indenes: potent and selective inhibitors of aldosterone synthase (CYP11B2) for the treatment of congestive heart failure and myocardia | 2006 | Journal of medicinal chemistry, Apr-06, Volume: 49, Issue:7 | Synthesis and evaluation of heteroaryl-substituted dihydronaphthalenes and indenes: potent and selective inhibitors of aldosterone synthase (CYP11B2) for the treatment of congestive heart failure and myocardial fibrosis. |
| AID1798554 | CYP11B1 Inhibition Assay from Article 10.1021/jm800355c: \\Synthesis, biological evaluation, and molecular modeling of abiraterone analogues: novel CYP17 inhibitors for the treatment of prostate cancer.\\ | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16 | Synthesis, biological evaluation, and molecular modeling of abiraterone analogues: novel CYP17 inhibitors for the treatment of prostate cancer. |
| AID1799837 | CYP24A1Inhibition Assay from Article 10.1021/bi101488p: \\Screening of selective inhibitors of 1a,25-dihydroxyvitamin D3 24-hydroxylase using recombinant human enzyme expressed in Escherichia coli.\\ | 2010 | Biochemistry, Dec-14, Volume: 49, Issue:49 | Screening of selective inhibitors of 1α,25-dihydroxyvitamin D3 24-hydroxylase using recombinant human enzyme expressed in Escherichia coli. |
| AID1798553 | CYP17 Inhibition Assay from Article 10.1021/jm800355c: \\Synthesis, biological evaluation, and molecular modeling of abiraterone analogues: novel CYP17 inhibitors for the treatment of prostate cancer.\\ | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16 | Synthesis, biological evaluation, and molecular modeling of abiraterone analogues: novel CYP17 inhibitors for the treatment of prostate cancer. |
| AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
| AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
| AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
| AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
| AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
| AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
| AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
| AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
| AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
| AID588461 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
| AID588461 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
| AID588461 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
| AID588460 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
| AID588460 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
| AID588460 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
| AID588459 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
| AID588459 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
| AID588459 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
| AID1508628 | Confirmatory qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
| AID1508627 | Counterscreen qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: GLuc-NoTag assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
| AID1508629 | Cell Viability qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
| AID1347411 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| AID540299 | A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis | 2010 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21 | Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis. |
| AID588519 | A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities | 2011 | Antiviral research, Sep, Volume: 91, Issue:3 | High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors. |
| AID1794808 | Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL). | 2014 | Journal of biomolecular screening, Jul, Volume: 19, Issue:6 | A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum. |
| AID1794808 | Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL). | |||
| AID1224864 | HCS microscopy assay (F508del-CFTR) | 2016 | PloS one, , Volume: 11, Issue:10 | Increasing the Endoplasmic Reticulum Pool of the F508del Allele of the Cystic Fibrosis Transmembrane Conductance Regulator Leads to Greater Folding Correction by Small Molecule Therapeutics. |
| AID750218 | Antifungal activity against Candida albicans NRRLY-477 after 24 hrs by two fold serial dilution technique | 2013 | European journal of medicinal chemistry, Jun, Volume: 64 | Thiourea derivatives incorporating a hippuric acid moiety: synthesis and evaluation of antibacterial and antifungal activities. |
| AID363953 | Antimicrobial activity against Cryptococcus neoformans IM 972751 isolate at 6.25 ug/ml after 48 hrs | 2008 | Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17 | In vitro antifungal activity of polyfunctionalized 2-(hetero)arylquinolines prepared through imino Diels-Alder reactions. |
| AID39394 | Minimum inhibitory concentration against Aspergillus flavus | 2004 | Bioorganic & medicinal chemistry letters, Feb-09, Volume: 14, Issue:3 | Synthesis and antifungal activities of phenylenedithioureas. |
| AID384955 | Intrinsic aqueous solubility at pH 10 by shake-flask method | 2008 | Journal of medicinal chemistry, May-22, Volume: 51, Issue:10 | Molecular characteristics for solid-state limited solubility. |
| AID1165072 | Inhibition of mouse CYP27B1 by cell-free assay | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | Novel styryl-indoles as small molecule inhibitors of 25-hydroxyvitamin D-24-hydroxylase (CYP24A1): Synthesis and biological evaluation. |
| AID493997 | Antifungal activity against Candida albicans ATCC 10231 assessed as inhibition of fungal growth at 200 uM | 2010 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 20, Issue:16 | New antifungal peptides. Synthesis, bioassays and initial structure prediction by CD spectroscopy. |
| AID419354 | Antifungal activity against Fusarium solani at 200 ug/disk after 48 hrs by agar disc-diffusion method | 2009 | European journal of medicinal chemistry, May, Volume: 44, Issue:5 | Synthesis and bioassay of a new class of heterocycles pyrrolyl oxadiazoles/thiadiazoles/triazoles. |
| AID635008 | Antifungal activity against Aspergillus niger NCIM 596 assessed as zone of inhibition at 100 ug/disc after 48 hrs by disk diffusion method | 2012 | European journal of medicinal chemistry, Jan, Volume: 47, Issue:1 | Synthesis, antimicrobial, antimycobacterial and structure-activity relationship of substituted pyrazolo-, isoxazolo-, pyrimido- and mercaptopyrimidocyclohepta[b]indoles. |
| AID367165 | Cytotoxicity against human Hep3B cells at 0.001 mg/ml | 2009 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 19, Issue:3 | Synthesis and antifungal activity of 1,2,3-triazole containing fluconazole analogues. |
| AID380257 | Antifungal activity against Fusarium oxysporum f. sp. vasinfectum by MTT assay | 2006 | Journal of natural products, Dec, Volume: 69, Issue:12 | Bioactive oligostilbenoids from the stem bark of Hopea exalata. |
| AID531183 | Antifungal activity against Candida albicans ATCC 32354 after 48 hrs by CLSI method | 2008 | Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7 | Potent in vitro antifungal activities of naturally occurring acetylenic acids. |
| AID582800 | Antifungal activity against Candida albicans isolate 488 harboring ERG3 H243N, T330A, A351V and ERG11 D225G, E266D, E391G, V488I mutant genes by broth microdilution method | 2010 | Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11 | Identification and characterization of four azole-resistant erg3 mutants of Candida albicans. |
| AID1061001 | Antimicrobial activity against Candida albicans CGMCC2.2086 after 48 hrs by twofold serial microdilution method | 2014 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1 | Synthesis and biological evaluation of novel N-substituted 1H-dibenzo[a,c]carbazole derivatives of dehydroabietic acid as potential antimicrobial agents. |
| AID681143 | TP_TRANSPORTER: increase in Calcein-AM intracellular accumulation in MDR1-expressing LLC-PK1 cells | 2002 | Molecular pharmacology, May, Volume: 61, Issue:5 | Three-dimensional quantitative structure-activity relationships of inhibitors of P-glycoprotein. |
| AID319751 | Antimicrobial activity against Cryptococcus parapsilosis isolates | 2008 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 18, Issue:11 | Synthesis and SAR studies of biaryloxy-substituted triazoles as antifungal agents. |
| AID530577 | Antileishmanial activity against Leishmania infantum promastigotes overexpressing LiABCG6 assessed as cell viability after 72 hrs by MTT assay | 2008 | Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10 | Characterization of an ABCG-like transporter from the protozoan parasite Leishmania with a role in drug resistance and transbilayer lipid movement. |
| AID664307 | Antifungal activity against Candida albicans MTCC 183 by agar streak dilution method | 2012 | European journal of medicinal chemistry, Jul, Volume: 53 | Synthesis of benzimidazolyl-1,3,4-oxadiazol-2ylthio-N-phenyl (benzothiazolyl) acetamides as antibacterial, antifungal and antituberculosis agents. |
| AID530981 | Antifungal activity against Candida albicans ATCC 200955 after 48 hrs by CLSI method | 2008 | Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7 | Potent in vitro antifungal activities of naturally occurring acetylenic acids. |
| AID1300881 | Antifungal activity against Candida krusei clinical isolate after 24 hrs by broth microdilution method | 2016 | European journal of medicinal chemistry, Jul-19, Volume: 117 | Novel 1,3-thiazolidin-4-one derivatives as promising anti-Candida agents endowed with anti-oxidant and chelating properties. |
| AID53234 | Inhibition of human testicular microsomal Cytochrome P450 17A1 | 1998 | Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6 | Novel 17-azolyl steroids, potent inhibitors of human cytochrome 17 alpha-hydroxylase-C17,20-lyase (P450(17) alpha): potential agents for the treatment of prostate cancer. |
| AID596527 | Antifungal activity against Microsporum gypseum C 115 2000 | 2011 | Bioorganic & medicinal chemistry, May-01, Volume: 19, Issue:9 | Antifungal, cytotoxic and SAR studies of a series of N-alkyl, N-aryl and N-alkylphenyl-1,4-pyrrolediones and related compounds. |
| AID688648 | Fungicidal activity against Penicillium chrysogenum after 48 hrs by broth dilution method | 2011 | European journal of medicinal chemistry, Nov, Volume: 46, Issue:11 | Synthesis and antimicrobial activity of amido linked pyrrolyl and pyrazolyl-oxazoles, thiazoles and imidazoles. |
| AID49459 | Antifungal activity in rat vaginal candidasis, 1 day postinfection with Candida. albicans SOB FM-391 | 1988 | Journal of medicinal chemistry, Oct, Volume: 31, Issue:10 | Studies on antifungal agents. 23. Novel substituted 3,5-diphenyl-3-(1H-imidazol-1-ylmethyl)- 2-alkylisoxazolidine derivatives. |
| AID405105 | Antimicrobial activity against Rhizopus microsporus var. rhizopodiformis assessed as percent of susceptible isolates after 24 hrs | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | In vitro susceptibilities of 217 clinical isolates of zygomycetes to conventional and new antifungal agents. |
| AID48787 | In vitro Minimum inhibitory concentration was determined by microbroth dilution assay on Candida tropicalis | 1992 | Journal of medicinal chemistry, Jan, Volume: 35, Issue:1 | Synthesis, specificity, and antifungal activity of inhibitors of the Candida albicans delta 24-sterol methyltransferase. |
| AID1068781 | Antifungal activity against Aspergillus niger at 50 ug/well after 48 hrs by agar well diffusion method | 2014 | European journal of medicinal chemistry, Feb-12, Volume: 73 | Synthesis and antimicrobial activity of (1,4-phenylene)bis(arylsulfonylpyrazoles and isoxazoles). |
| AID403694 | Antifungal activity against Candida tropicalis after 48 hrs by spectrophotometry | 2005 | Journal of natural products, Oct, Volume: 68, Issue:10 | Steroidal saponins from Smilax medica and their antifungal activity. |
| AID1068780 | Antifungal activity against Penicillium chrysogenum at 50 ug/well after 48 hrs by agar well diffusion method | 2014 | European journal of medicinal chemistry, Feb-12, Volume: 73 | Synthesis and antimicrobial activity of (1,4-phenylene)bis(arylsulfonylpyrazoles and isoxazoles). |
| AID420214 | Antimicrobial activity against Micrococcus luteus UFPEDA 06 after 20 hrs by twofold serial dilution technique | 2009 | European journal of medicinal chemistry, May, Volume: 44, Issue:5 | Synthesis, antimicrobial and cytotoxic activities of some 5-arylidene-4-thioxo-thiazolidine-2-ones. |
| AID48251 | Inhibitory activity against Candida. species (40 clinical isolates), determined at pH-5.8 | 1995 | Journal of medicinal chemistry, Oct-13, Volume: 38, Issue:21 | Antifungal agents. 9. 3-Aryl-4-[alpha-(1H-imidazol-1-yl)arylmethyl]pyrroles: a new class of potent anti-Candida agents. |
| AID1191386 | Inhibition of human recombinant CYP17 expressed in Escherichia coli using progesterone as substrate | 2015 | European journal of medicinal chemistry, Jan-27, Volume: 90 | Heteroatom insertion into 3,4-dihydro-1H-quinolin-2-ones leads to potent and selective inhibitors of human and rat aldosterone synthase. |
| AID633917 | Antifungal activity against Aspergillus fumigatus ATCC 28212 by twofold serial dilution technique | 2012 | European journal of medicinal chemistry, Jan, Volume: 47, Issue:1 | Isoxazoles incorporated N-substituted decahydroquinolines: a precursor to the next generation antimicrobial drug. |
| AID515012 | Antifungal activity against Candida tropicalis by micro-broth dilution method | 2010 | European journal of medicinal chemistry, Oct, Volume: 45, Issue:10 | Synthesis and antifungal evaluation of novel triazole derivatives as inhibitors of cytochrome P450 14alpha-demethylase. |
| AID514964 | Inhibition of CYP24A1 expressed in CHO cells | 2010 | European journal of medicinal chemistry, Oct, Volume: 45, Issue:10 | Synthesis and CYP24A1 inhibitory activity of (E)-2-(2-substituted benzylidene)- and 2-(2-substituted benzyl)-6-methoxy-tetralones. |
| AID1312610 | Antifungal activity against naftifine-sensitive Trichophyton verrucosum after 7 days by serial dilution method | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10 | Discovery of Benzocycloalkane Derivatives Efficiently Blocking Bacterial Virulence for the Treatment of Methicillin-Resistant S. aureus (MRSA) Infections by Targeting Diapophytoene Desaturase (CrtN). |
| AID636993 | Antifungal activity against Candida albicans after 48 hrs by agar streak dilution method | 2012 | European journal of medicinal chemistry, Feb, Volume: 48 | Synthesis and biological evaluation of some thiazolidinones as antimicrobial agents. |
| AID1328091 | Antibacterial activity against Klebsiella pneumoniae after 24 hrs by broth dilution method | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | Synthesis and antimicrobial activity of styryl/pyrrolyl/pyrazolyl sulfonylmethyl-1,3,4-oxadiazolyl amines and styryl/pyrrolyl/pyrazolyl sulfonylmethyl-1,3,4-thiadiazolyl amines. |
| AID2947 | Inhibition of 17-alpha-hydroxylase/17,20 lyase from rat testes microsomal preparation | 1990 | Journal of medicinal chemistry, Sep, Volume: 33, Issue:9 | Hydroxyperfluoroazobenzenes: novel inhibitors of enzymes of androgen biosynthesis. |
| AID481911 | Antifungal activity against Candida albicans ATCC 12983 at 15 ug in 6 mm disk after 10 hrs by disc-diffusion assay | 2010 | Journal of natural products, May-28, Volume: 73, Issue:5 | Chemical epigenetics alters the secondary metabolite composition of guttate excreted by an atlantic-forest-soil-derived Penicillium citreonigrum. |
| AID680014 | TP_TRANSPORTER: inhibition of Fexofenadine uptake (Fexofenadine: 2 uM, Ketoconazole: 100 uM) in Xenopus laevis oocytes | 1999 | Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 27, Issue:8 | OATP and P-glycoprotein transporters mediate the cellular uptake and excretion of fexofenadine. |
| AID600780 | Fungicidal activity against Fusarium sporotrichioides IMT 496 after 72 hrs | 2011 | Bioorganic & medicinal chemistry, May-15, Volume: 19, Issue:10 | Thiazole-based chalcones as potent antimicrobial agents. Synthesis and biological evaluation. |
| AID376049 | Antifungal activity against Candida albicans ATCC 10231 by agar dilution method | 1999 | Journal of natural products, Oct, Volume: 62, Issue:10 | In vitro evaluation of antifungal properties of phenylpropanoids and related compounds acting against dermatophytes. |
| AID48058 | The compound was tested for antifungal activity against Candida parapsilosis MY1010 using agar dilution assay | 1987 | Journal of medicinal chemistry, Aug, Volume: 30, Issue:8 | Lysosomotropic agents. 7. Broad-spectrum antifungal activity of lysosomotropic detergents. |
| AID367158 | Antimicrobial activity against Cryptococcus neoformans by broth microdilution method | 2009 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 19, Issue:3 | Synthesis and antifungal activity of 1,2,3-triazole containing fluconazole analogues. |
| AID394826 | Antitrypanosomal activity against Trypanosoma cruzi Tulahuen amastigotes expressing beta-galactosidase in mouse 3T3 fibroblast after 7 days by alamar blue assay | 2009 | Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6 | Rational modification of a candidate cancer drug for use against Chagas disease. |
| AID1221957 | Apparent permeability from basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2 | Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
| AID1057772 | Antimicrobial activity against Candida albicans ATCC 90028 after 24 hrs by broth microdilution method | 2013 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24 | Synthesis and initial biological evaluation of substituted 1-phenylamino-2-thio-4,5-dimethyl-1H-imidazole derivatives. |
| AID1110746 | Antifungal activity against Candida albicans ATCC 44859 after 48 hr by microdilution broth method | 2002 | Farmaco (Societa chimica italiana : 1989), Feb, Volume: 57, Issue:2 | Ring substituted 3-phenyl-1-(2-pyrazinyl)-2-propen-1-ones as potential photosynthesis-inhibiting, antifungal and antimycobacterial agents. |
| AID330535 | Antifungal activity against Candida parapsilosis infected cyclophosphamide-immunocompromized Crl:CD1(ICR) mouse assessed as fungal density in brain at 10 mg/kg, po for 5 days measured on day 12 | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Mar-13, Volume: 104, Issue:11 | High-throughput synergy screening identifies microbial metabolites as combination agents for the treatment of fungal infections. |
| AID49093 | The compound was tested for antifungal activity against Candida albicans MY1013 using agar dilution assay | 1987 | Journal of medicinal chemistry, Aug, Volume: 30, Issue:8 | Lysosomotropic agents. 7. Broad-spectrum antifungal activity of lysosomotropic detergents. |
| AID515015 | Antifungal activity against Aspergillus fumigatus by micro-broth dilution method | 2010 | European journal of medicinal chemistry, Oct, Volume: 45, Issue:10 | Synthesis and antifungal evaluation of novel triazole derivatives as inhibitors of cytochrome P450 14alpha-demethylase. |
| AID755105 | Inhibition of CYP3A4/5 in human intestinal microsomes using midazolam as substrate after 4 mins | 2013 | Bioorganic & medicinal chemistry, Jul-01, Volume: 21, Issue:13 | Semisynthesis, cytotoxicity, antiviral activity, and drug interaction liability of 7-O-methylated analogues of flavonolignans from milk thistle. |
| AID1209456 | Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1 | In vitro inhibition of the bile salt export pump correlates with risk of cholestatic drug-induced liver injury in humans. |
| AID530970 | Antifungal activity against Fluconazole resistant Candida albicans clinical isolate 1 after 48 hrs by CLSI method | 2008 | Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7 | Potent in vitro antifungal activities of naturally occurring acetylenic acids. |
| AID1429859 | n-octanol-phosphate buffer distribution coefficient, log D of the compound at pH 7.4 after 90 mins by shake-flask method | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Crystal structures, binding interactions, and ADME evaluation of brain penetrant N-substituted indazole-5-carboxamides as subnanomolar, selective monoamine oxidase B and dual MAO-A/B inhibitors. |
| AID456836 | Antifungal activity against Penicillium ochrochloron ATCC 9112 after 72 hrs by serial dilution method | 2010 | Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1 | Novel 4-thiazolidinone derivatives as potential antifungal and antibacterial drugs. |
| AID372241 | Fungistatic activity against Candida albicans SSK21 after 24 to 48 hrs by broth microdilution assay | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10 | The Ssk1p response regulator and Chk1p histidine kinase mutants of Candida albicans are hypersensitive to fluconazole and voriconazole. |
| AID1130392 | Antifungal activity against Sporothrix schenckii assessed as growth inhibition in sabouraud broth after 14 days in presence of 10% inactivated bovine serum | 1979 | Journal of medicinal chemistry, Aug, Volume: 22, Issue:8 | Antimycotic imidazoles. part 4. Synthesis and antifungal activity of ketoconazole, a new potent orally active broad-spectrum antifungal agent. |
| AID486233 | Selectivity index, ratio of ID50 for mouse J774 cells to ID50 for Trypanosoma cruzi Tulahuen 2 | 2010 | European journal of medicinal chemistry, Jun, Volume: 45, Issue:6 | Naftifine-analogues as anti-Trypanosoma cruzi agents. |
| AID405093 | Antimicrobial activity against Rhizopus arrhizus after 24 hrs | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | In vitro susceptibilities of 217 clinical isolates of zygomycetes to conventional and new antifungal agents. |
| AID262547 | Antifungal activity against Candida parapsilosis | 2006 | Journal of medicinal chemistry, Apr-20, Volume: 49, Issue:8 | Structure-based optimization of azole antifungal agents by CoMFA, CoMSIA, and molecular docking. |
| AID45343 | In vitro antifungal activity against 40 strains at pH 7.2 | 2002 | Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13 | Antifungal agents. 10. New derivatives of 1-[(aryl)[4-aryl-1H-pyrrol-3-yl]methyl]-1H-imidazole, synthesis, anti-candida activity, and quantitative structure-analysis relationship studies. |
| AID405111 | Antimicrobial activity against Absidia corymbifera assessed as percent of susceptible isolates after 24 hrs | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | In vitro susceptibilities of 217 clinical isolates of zygomycetes to conventional and new antifungal agents. |
| AID624622 | Apparent permeability (Papp) from apical to basolateral side determined in MDR1-MDCKII cells | 2001 | The Journal of pharmacology and experimental therapeutics, Nov, Volume: 299, Issue:2 | Rational use of in vitro P-glycoprotein assays in drug discovery. |
| AID282368 | Inhibition of ATRA-induced CYP26 in human T47D cells assessed as ATRA metabolism using [11.12-3H]-ATRA | 2004 | Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27 | Novel retinoic acid metabolism blocking agents endowed with multiple biological activities are efficient growth inhibitors of human breast and prostate cancer cells in vitro and a human breast tumor xenograft in nude mice. |
| AID432800 | Antifungal activity against Sporothrix schenckii after 72 hrs by microdilution method | 2008 | Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2 | In vitro antifungal susceptibilities of five species of sporothrix. |
| AID341763 | AUC (0 to tau) in human plasma at 200 mg qd for 4 days | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8 | Fosamprenavir plus ritonavir increases plasma ketoconazole and ritonavir exposure, while amprenavir exposure remains unchanged. |
| AID678720 | Metabolic stability in human liver microsomes assessed as low signal/noise ratio (S/N of 1 to 10) by measuring GSH adduct formation at 100 uM after 90 mins by HPLC-MS analysis | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
| AID1129507 | Antimicrobial activity against Aspergillus niger at 25 ug/well after 48 hrs by agar well diffusion method | 2014 | European journal of medicinal chemistry, Apr-22, Volume: 77 | Synthesis, antimicrobial and cytotoxic activities of pyrimidinyl benzoxazole, benzothiazole and benzimidazole. |
| AID490995 | Antifungal activity against Aspergillus niger at 100 ug/disk after 48 hrs by disk diffusion method | 2010 | European journal of medicinal chemistry, Jul, Volume: 45, Issue:7 | Synthesis and bioassay of pyrrolyl oxazolines and thiazolines. |
| AID284087 | Antifungal activity against Candida albicans C126-2000 after 48 hrs | 2007 | Bioorganic & medicinal chemistry, Jan-01, Volume: 15, Issue:1 | Synthesis and antifungal activity of (Z)-5-arylidenerhodanines. |
| AID1068769 | Antifungal activity against Penicillium chrysogenum after 48 hrs by broth dilution test | 2014 | European journal of medicinal chemistry, Feb-12, Volume: 73 | Synthesis and antimicrobial activity of (1,4-phenylene)bis(arylsulfonylpyrazoles and isoxazoles). |
| AID1157291 | Antifungal activity against Candida albicans SC5314 assessed as growth inhibition by automatic microplate reader analysis | 2014 | Journal of natural products, May-23, Volume: 77, Issue:5 | Polyhydroxy cyclohexanols from a Dendrodochium sp. fungus associated with the sea cucumber Holothuria nobilis Selenka. |
| AID218568 | Compound was tested for the inhibition beta-lactamase with 0.1 mg/ml saponin:No inhibition | 2003 | Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21 | Identification and prediction of promiscuous aggregating inhibitors among known drugs. |
| AID125961 | Minimum inhibitory concentration Microsporum gypseum | 2004 | Bioorganic & medicinal chemistry letters, Feb-09, Volume: 14, Issue:3 | Synthesis and antifungal activities of phenylenedithioureas. |
| AID1171978 | Antibacterial activity against Shigella flexneri MTCC 1457 assessed as zone of inhibition at 1 mg/disc after 24 hrs by disc diffusion method | 2015 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2 | Facile and diastereoselective synthesis of 3,2'-spiropyrrolidine-oxindoles derivatives, their molecular docking and antiproliferative activities. |
| AID228090 | In vivo activity against vaginal candidoses in rats, measured as the ratio of animals cured/animals infected (C/I) at dose 10 mg/kg; 173/181 | 1984 | Journal of medicinal chemistry, Jul, Volume: 27, Issue:7 | Antimycotic azoles. 7. Synthesis and antifungal properties of a series of novel triazol-3-ones. |
| AID1103208 | Antifungal activity against Colletotrichum truncatum CE175 after 48 to 72 hr | 2004 | Journal of agricultural and food chemistry, Jun-02, Volume: 52, Issue:11 | Antifungal chalcones and new caffeic acid esters from Zuccagnia punctata acting against soybean infecting fungi. |
| AID511863 | Antifungal activity against Candida sp. UFPEDA 2224 after 24 to 48 hrs by serial dilution method | 2010 | European journal of medicinal chemistry, Sep, Volume: 45, Issue:9 | Synthesis and evaluation of anti-Toxoplasma gondii and antimicrobial activities of thiosemicarbazides, 4-thiazolidinones and 1,3,4-thiadiazoles. |
| AID666781 | Antifungal activity against Septoria tritici at 0.05 mg by agar diffusion test | 2012 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 22, Issue:13 | Bioactive briarane diterpenoids from the South China Sea gorgonian Dichotella gemmacea. |
| AID391497 | Antifungal activity against Aspergillus fumigatus ATCC 26934 after 48 hrs by spectrophotometry | 2008 | Journal of natural products, Oct, Volume: 71, Issue:10 | Evidence for the mechanism of action of the antifungal phytolaccoside B isolated from Phytolacca tetramera Hauman. |
| AID616874 | Antimicrobial activity against Escherichia coli after 24 hrs by agar dilution method | 2011 | Journal of natural products, Aug-26, Volume: 74, Issue:8 | Cytotoxic bipyridines from the marine-derived actinomycete Actinoalloteichus cyanogriseus WH1-2216-6. |
| AID405097 | Antimicrobial activity against Absidia sp. after 24 hrs | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | In vitro susceptibilities of 217 clinical isolates of zygomycetes to conventional and new antifungal agents. |
| AID588215 | FDA HLAED, alkaline phosphatase increase | 2004 | Current drug discovery technologies, Dec, Volume: 1, Issue:4 | Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling. |
| AID48271 | Tested In vitro for antifungal activity against candida Spp (Candida glabrata, Candida krusei) at pH 7.2 | 2002 | Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13 | Antifungal agents. 10. New derivatives of 1-[(aryl)[4-aryl-1H-pyrrol-3-yl]methyl]-1H-imidazole, synthesis, anti-candida activity, and quantitative structure-analysis relationship studies. |
| AID45473 | In vitro antifungal activity against Candida albicans ATCC 10259 | 1988 | Journal of medicinal chemistry, Oct, Volume: 31, Issue:10 | Studies on antifungal agents. 23. Novel substituted 3,5-diphenyl-3-(1H-imidazol-1-ylmethyl)- 2-alkylisoxazolidine derivatives. |
| AID47584 | Evaluation of In vitro antifungal activity against Candida albicans ATCC 10231 by broth macro dilution method | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20 | Synthesis and antifungal activity of new azole derivatives containing an N-acylmorpholine ring. |
| AID214094 | In vitro antifungal activity against Trichophyton mentagrophytes | 1984 | Journal of medicinal chemistry, Jul, Volume: 27, Issue:7 | Antimycotic azoles. 7. Synthesis and antifungal properties of a series of novel triazol-3-ones. |
| AID533805 | Antifungal activity against Trichophyton rubrum C137 by agar dilution method | 2010 | European journal of medicinal chemistry, Nov, Volume: 45, Issue:11 | Synthesis and biological evaluation of N-antipyrine-4-substituted amino-3-chloromaleimide derivatives. |
| AID406951 | Antifungal activity against Candida albicans ATCC 10261 at 35 degC after 48 hrs by broth microdilution test | 2008 | Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13 | 1-[(3-Aryloxy-3-aryl)propyl]-1H-imidazoles, new imidazoles with potent activity against Candida albicans and dermatophytes. Synthesis, structure-activity relationship, and molecular modeling studies. |
| AID511862 | Antifungal activity against Candida albicans UFPEDA 1007 after 24 to 48 hrs by serial dilution method | 2010 | European journal of medicinal chemistry, Sep, Volume: 45, Issue:9 | Synthesis and evaluation of anti-Toxoplasma gondii and antimicrobial activities of thiosemicarbazides, 4-thiazolidinones and 1,3,4-thiadiazoles. |
| AID644189 | Antifungal activity against Penicillium ochrochloron ATCC 9112 treated for 72 hrs followed by sub-cultivated for 5 days by serial dilution method | 2012 | Bioorganic & medicinal chemistry, Feb-15, Volume: 20, Issue:4 | Synthesis of novel sulfonamide-1,2,4-triazoles, 1,3,4-thiadiazoles and 1,3,4-oxadiazoles, as potential antibacterial and antifungal agents. Biological evaluation and conformational analysis studies. |
| AID363943 | Antimicrobial activity against Cryptococcus neoformans IM 983036 isolate at 6.25 ug/ml after 48 hrs | 2008 | Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17 | In vitro antifungal activity of polyfunctionalized 2-(hetero)arylquinolines prepared through imino Diels-Alder reactions. |
| AID364067 | Antifungal activity against Trichophyton rubrum ATCC 10218 after 48 hrs by MTT assay | 2008 | European journal of medicinal chemistry, Sep, Volume: 43, Issue:9 | Enamines as novel antibacterials and their structure-activity relationships. |
| AID659909 | Antifungal activity against Saccharomyces cerevisiae by two-fold serial dilution method | 2012 | European journal of medicinal chemistry, Jun, Volume: 52 | Design and synthesis of new 4-pyrazolin-3-yl-1,2,3-triazoles and 1,2,3-triazol-4-yl-pyrazolin-1-ylthiazoles as potential antimicrobial agents. |
| AID554718 | Antimicrobial activity against Saccharomyces cerevisiae isolate ADdelta overexpressing Saccharomyces cerevisiae ERG11 after 48 hrs by liquid microdilution assay | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2 | Abc1p is a multidrug efflux transporter that tips the balance in favor of innate azole resistance in Candida krusei. |
| AID243151 | Inhibitory concentration against potassium channel HERG | 2005 | Bioorganic & medicinal chemistry letters, Jun-02, Volume: 15, Issue:11 | A discriminant model constructed by the support vector machine method for HERG potassium channel inhibitors. |
| AID54782 | Inhibition of recombinant human Cytochrome P450 3A4 with BFC [7-benzyloxy-4-trifluoromethylcoumarin] after 45 minutes | 2003 | Journal of medicinal chemistry, Aug-28, Volume: 46, Issue:18 | Fluorine substitution can block CYP3A4 metabolism-dependent inhibition: identification of (S)-N-[1-(4-fluoro-3- morpholin-4-ylphenyl)ethyl]-3- (4-fluorophenyl)acrylamide as an orally bioavailable KCNQ2 opener devoid of CYP3A4 metabolism-dependent inhibiti |
| AID1061738 | Antimicrobial activity against Trichophyton rubrum by broth microdilution method | 2014 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1 | Synthesis and evaluation of novel azoles as potent antifungal agents. |
| AID560138 | Antifungal activity against Candida glabrata isolate 22852 at 10 ug after 48 hrs by disk diffusion method | 2009 | Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7 | Hypersusceptibility to azole antifungals in a clinical isolate of Candida glabrata with reduced aerobic growth. |
| AID260490 | Opening large conductance calcium-activated potassium channel in bovine smooth muscle cells at 30 uM | 2006 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 16, Issue:4 | Partial structures of ketoconazole as modulators of the large conductance calcium-activated potassium channel (BK(Ca)). |
| AID1171975 | Antibacterial activity against Salmonella typhimurium MTCC 1251 assessed as zone of inhibition at 1 mg/disc after 24 hrs by disc diffusion method | 2015 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2 | Facile and diastereoselective synthesis of 3,2'-spiropyrrolidine-oxindoles derivatives, their molecular docking and antiproliferative activities. |
| AID220094 | The compound was evaluated for mean zone diameter (inhibition) against yeast at the concentration of 125 ug/mL | 1987 | Journal of medicinal chemistry, Aug, Volume: 30, Issue:8 | Lysosomotropic agents. 7. Broad-spectrum antifungal activity of lysosomotropic detergents. |
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| AID343557 | Antitrypanosomal activity against epimastigotes of Trypanosoma cruzi Tulahuen 2 | 2008 | Bioorganic & medicinal chemistry, Jul-15, Volume: 16, Issue:14 | New trypanocidal hybrid compounds from the association of hydrazone moieties and benzofuroxan heterocycle. |
| AID1066221 | Inhibition of CYP3A4 (unknown origin) by fluorescence assay | 2014 | Journal of medicinal chemistry, Jan-09, Volume: 57, Issue:1 | Discovery of a non-estrogenic irreversible inhibitor of 17β-hydroxysteroid dehydrogenase type 1 from 3-substituted-16β-(m-carbamoylbenzyl)-estradiol derivatives. |
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| AID330536 | Antifungal activity against Candida parapsilosis infected cyclophosphamide-immunocompromized Crl:CD1(ICR) mouse assessed as fungal density in brain at 50 mg/kg, po for 5 days measured on day 12 | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Mar-13, Volume: 104, Issue:11 | High-throughput synergy screening identifies microbial metabolites as combination agents for the treatment of fungal infections. |
| AID611682 | Antifungal activity against Microbotryum violaceum at 0.05 mg by agar diffusion method | 2011 | Journal of natural products, Jul-22, Volume: 74, Issue:7 | Bioactive 11,20-epoxy-3,5(16)-diene briarane diterpenoids from the South China Sea gorgonian Dichotella gemmacea. |
| AID391495 | Antifungal activity against Saccharomyces cerevisiae ATCC 9763 after 48 hrs by sorbitol protection assay by spectrophotometry | 2008 | Journal of natural products, Oct, Volume: 71, Issue:10 | Evidence for the mechanism of action of the antifungal phytolaccoside B isolated from Phytolacca tetramera Hauman. |
| AID1467469 | Antifungal activity against Fusarium moniliforme at 100 ug/ml after 48 hrs by agar well diffusion method | 2017 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 27, Issue:14 | Synthesis, SAR and molecular docking studies of benzo[d]thiazole-hydrazones as potential antibacterial and antifungal agents. |
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| AID1312608 | Antifungal activity against naftifine-sensitive Microsporum gypseum after 7 days by serial dilution method | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10 | Discovery of Benzocycloalkane Derivatives Efficiently Blocking Bacterial Virulence for the Treatment of Methicillin-Resistant S. aureus (MRSA) Infections by Targeting Diapophytoene Desaturase (CrtN). |
| AID420067 | Antifungal activity against Candida albicans CA-6 after 24 hrs by broth microdilution assay | 2009 | Bioorganic & medicinal chemistry, Jun-01, Volume: 17, Issue:11 | Bulky 1,4-benzoxazine derivatives with antifungal activity. |
| AID468470 | Antimicrobial activity against Cryptococcus neoformans ATCC 24067D2 after 48 hrs | 2010 | European journal of medicinal chemistry, Mar, Volume: 45, Issue:3 | Synthesis, characterization and biocidal activity of new organotin complexes of 2-(3-oxocyclohex-1-enyl)benzoic acid. |
| AID261014 | Inhibitory activity against Candida tropicalis | 2006 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 16, Issue:4 | Novel endoperoxides: synthesis and activity against Candida species. |
| AID530961 | Antifungal activity against Candida parapsilosis ATCC 22019 after 48 hrs by CLSI method | 2008 | Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7 | Potent in vitro antifungal activities of naturally occurring acetylenic acids. |
| AID325036 | Antimicrobial activity against Candida albicans P5 after 24 hrs by broth macrodilution method | 2007 | Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5 | A Candida albicans petite mutant strain with uncoupled oxidative phosphorylation overexpresses MDR1 and has diminished susceptibility to fluconazole and voriconazole. |
| AID1171981 | Antibacterial activity against Staphylococcus epidermidis MTCC 3615 assessed as zone of inhibition at 1 mg/disc after 24 hrs by disc diffusion method | 2015 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2 | Facile and diastereoselective synthesis of 3,2'-spiropyrrolidine-oxindoles derivatives, their molecular docking and antiproliferative activities. |
| AID214280 | Minimum inhibitory concentration against Trichophyton mentagrophytes | 2004 | Bioorganic & medicinal chemistry letters, Feb-09, Volume: 14, Issue:3 | Synthesis and antifungal activities of phenylenedithioureas. |
| AID54780 | Inhibition of recombinant human Cytochrome P450 3A4 with BFC [7-benzyloxy-4-trifluoromethylcoumarin] after 15 minutes | 2003 | Journal of medicinal chemistry, Aug-28, Volume: 46, Issue:18 | Fluorine substitution can block CYP3A4 metabolism-dependent inhibition: identification of (S)-N-[1-(4-fluoro-3- morpholin-4-ylphenyl)ethyl]-3- (4-fluorophenyl)acrylamide as an orally bioavailable KCNQ2 opener devoid of CYP3A4 metabolism-dependent inhibiti |
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| AID1217576 | Half life in castrated pig plasma withdrawn from femoral vein at 200 mg/kg dosed via intrajejunal route by UPLC-tandem mass spectrometry | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5 | In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole. |
| AID125951 | Minimum inhibitory concentration against Microsporum cookei | 2004 | Bioorganic & medicinal chemistry letters, Feb-09, Volume: 14, Issue:3 | Synthesis and antifungal activities of phenylenedithioureas. |
| AID294854 | Antifungal activity against Fonsecaea compacta after 7 days by micro-broth dilution method | 2007 | European journal of medicinal chemistry, Sep, Volume: 42, Issue:9 | Synthesis of novel triazole derivatives as inhibitors of cytochrome P450 14alpha-demethylase (CYP51). |
| AID648036 | Antifungal activity against Candida albicans NRRL Y-477 by two fold serial dilution method | 2012 | European journal of medicinal chemistry, Apr, Volume: 50 | Regioselective synthesis and antimicrobial activities of some novel aryloxyacetic acid derivatives. |
| AID1177651 | Inhibition of human aldosterone synthase expressed in V79 MZ cells | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12 | Aldosterone synthase inhibitors as promising treatments for mineralocorticoid dependent cardiovascular and renal diseases. |
| AID494182 | Antimicrobial activity against Candida glabrata by broth microdilution method | 2010 | European journal of medicinal chemistry, Aug, Volume: 45, Issue:8 | Antimicrobial activity and a SAR study of some novel benzimidazole derivatives bearing hydrazone moiety. |
| AID290148 | Antifungal activity against Aspergillus niger after 48 hrs by MTT colorimetric method | 2007 | European journal of medicinal chemistry, Apr, Volume: 42, Issue:4 | Synthesis and antimicrobial activities of Schiff bases derived from 5-chloro-salicylaldehyde. |
| AID674802 | Antifungal activity against wild type Aspergillus flavus NRRL3357 after 48 hrs by microtiter broth dilution method | 2012 | European journal of medicinal chemistry, Sep, Volume: 55 | Laurene-type sesquiterpenes from the Red Sea red alga Laurencia obtusa as potential antitumor-antimicrobial agents. |
| AID1129513 | Antimicrobial activity against Staphylococcus aureus ATCC 25923 after 24 hrs by broth dilution method | 2014 | European journal of medicinal chemistry, Apr-22, Volume: 77 | Synthesis, antimicrobial and cytotoxic activities of pyrimidinyl benzoxazole, benzothiazole and benzimidazole. |
| AID533800 | Antifungal activity against Aspergillus fumigatus ATCC 26934 by agar dilution method | 2010 | European journal of medicinal chemistry, Nov, Volume: 45, Issue:11 | Synthesis and biological evaluation of N-antipyrine-4-substituted amino-3-chloromaleimide derivatives. |
| AID54929 | Inhibition of lanosterol 14 alpha-demethylase cytochrome P450 51A | 1992 | Journal of medicinal chemistry, Jul-24, Volume: 35, Issue:15 | Stereoisomers of ketoconazole: preparation and biological activity. |
| AID43564 | Effect of pre-incubation with enzyme on the inhibition of beta-lactamase:No inhibition | 2003 | Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21 | Identification and prediction of promiscuous aggregating inhibitors among known drugs. |
| AID491001 | Antifungal activity against Fusarium solani after 48 hrs by microdilution susceptibility assay | 2010 | European journal of medicinal chemistry, Jul, Volume: 45, Issue:7 | Synthesis and bioassay of pyrrolyl oxazolines and thiazolines. |
| AID555137 | Antimicrobial activity against Candida parapsilosis ATCC 22019 by CLSI M27-A2 broth microdilution method | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Fenticonazole activity measured by the methods of the European Committee on Antimicrobial Susceptibility Testing and CLSI against 260 Candida vulvovaginitis isolates from two European regions and annotations on the prevalent genotypes. |
| AID1079947 | Comments (NB not yet translated). [column 'COMMENTAIRES' in source] | |||
| AID47864 | Evaluation of In vitro antifungal activity against Candida parapsilosis 2.07 by broth macro dilution method | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20 | Synthesis and antifungal activity of new azole derivatives containing an N-acylmorpholine ring. |
| AID284094 | Antifungal activity against Candida lusitaniae C131-2000 after 48 hrs | 2007 | Bioorganic & medicinal chemistry, Jan-01, Volume: 15, Issue:1 | Synthesis and antifungal activity of (Z)-5-arylidenerhodanines. |
| AID313550 | Inhibition of hepatic CYP1A2 at 10 uM | 2008 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 18, Issue:1 | Synthesis, biological evaluation and molecular modelling studies of novel ACD- and ABD-ring steroidomimetics as inhibitors of CYP17. |
| AID1075574 | Antimicrobial activity against Trichoderma harzianum NRRL 20565 after 48 to 72 hrs by microbroth dilution method | 2014 | European journal of medicinal chemistry, Mar-03, Volume: 74 | Synthesis and biological evaluation of thiazoline derivatives as new antimicrobial and anticancer agents. |
| AID319756 | Antimicrobial activity against Microsporum gypseum isolates | 2008 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 18, Issue:11 | Synthesis and SAR studies of biaryloxy-substituted triazoles as antifungal agents. |
| AID560240 | Antifungal activity against Candida albicans by checkerboard method in presence of miconazole | 2009 | Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8 | Curcumin modulates efflux mediated by yeast ABC multidrug transporters and is synergistic with antifungals. |
| AID613256 | Antibacterial activity against Staphylococcus aureus ATCC 10832 after 24 hrs by NCCLS M7-A6 broth dilution method | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Design, synthesis and antimicrobial activity of chiral 2-(substituted-hydroxyl)-3-(benzo[d]oxazol-5-yl)propanoic acid derivatives. |
| AID681138 | TP_TRANSPORTER: increase in Calcein-AM intracellular accumulation in mdr1b-expressing LLC-PK1 cells | 2002 | The Journal of pharmacology and experimental therapeutics, Oct, Volume: 303, Issue:1 | Interaction of cytochrome P450 3A inhibitors with P-glycoprotein. |
| AID1129512 | Antimicrobial activity against Penicillium chrysogenum at 100 ug/well after 48 hrs by agar well diffusion method | 2014 | European journal of medicinal chemistry, Apr-22, Volume: 77 | Synthesis, antimicrobial and cytotoxic activities of pyrimidinyl benzoxazole, benzothiazole and benzimidazole. |
| AID355710 | Antifungal activity against Candida albicans MSU-SM 543 after 2 to 4 days | |||
| AID596444 | Antifungal activity against Candida tropicalis C 131 2000 | 2011 | Bioorganic & medicinal chemistry, May-01, Volume: 19, Issue:9 | Antifungal, cytotoxic and SAR studies of a series of N-alkyl, N-aryl and N-alkylphenyl-1,4-pyrrolediones and related compounds. |
| AID419363 | Antifungal activity against Fusarium solani after 48 hrs by microdilution susceptibility method | 2009 | European journal of medicinal chemistry, May, Volume: 44, Issue:5 | Synthesis and bioassay of a new class of heterocycles pyrrolyl oxadiazoles/thiadiazoles/triazoles. |
| AID625291 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID302125 | Antifungal activity against fluconazole-resistant Candida albicans 25 after 24 hrs | 2007 | Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22 | Synthesis and antifungal activities of novel 2-aminotetralin derivatives. |
| AID574269 | Antifungal activity against 48 hrs cultures of 10'7 cells/ml biofilm-derived Candida albicans ATCC 90028 planktonic cells hrs by XTT reduction method | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | Cell density and cell aging as factors modulating antifungal resistance of Candida albicans biofilms. |
| AID456684 | Antifungal activity against Cryptococcus neoformans ATCC 32264 assessed as inhibition of fungal growth at 25 uM after 48 hrs by microbroth dilution method | 2010 | Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1 | New small-size peptides possessing antifungal activity. |
| AID228100 | In vivo activity against vaginal candidoses in rats, measured as the ratio of animals cured/animals infected (C/I) at dose 2.5 mg/kg; 2/8 | 1984 | Journal of medicinal chemistry, Jul, Volume: 27, Issue:7 | Antimycotic azoles. 7. Synthesis and antifungal properties of a series of novel triazol-3-ones. |
| AID687503 | Antifungal activity against Aspergillus flavus ATCC 9170 by NCCLS broth microdilution method | 2012 | Bioorganic & medicinal chemistry, Oct-15, Volume: 20, Issue:20 | Structure-activity relationship study of nitrosopyrimidines acting as antifungal agents. |
| AID576612 | Inhibition of human ERG | 2011 | European journal of medicinal chemistry, Feb, Volume: 46, Issue:2 | Predicting hERG activities of compounds from their 3D structures: development and evaluation of a global descriptors based QSAR model. |
| AID323062 | Antifungal activity against Aspergillus flavus ATCC 9170 by micro-broth dilution method | 2008 | Bioorganic & medicinal chemistry, Jan-15, Volume: 16, Issue:2 | Antifungal and cytotoxic activities of some N-substituted aniline derivatives bearing a hetaryl fragment. |
| AID42856 | Inhibition of Candida albicans ATCC 44859 growth for 48 hours in vitro. | 2001 | Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17 | 3-Phenyl-5-acyloxymethyl-2H,5H-furan-2-ones: synthesis and biological activity of a novel group of potential antifungal drugs. |
| AID1328085 | Antifungal activity against Penicillium chrysogenum assessed as inhibition of spore germination at 100 ug/well after 48 hrs by agar well diffusion method | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | Synthesis and antimicrobial activity of styryl/pyrrolyl/pyrazolyl sulfonylmethyl-1,3,4-oxadiazolyl amines and styryl/pyrrolyl/pyrazolyl sulfonylmethyl-1,3,4-thiadiazolyl amines. |
| AID86932 | Percentage lowering of the total serum cholesterol in male hamsters at a dose of 50 mg/dL orally administered for 14 days | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | Selective inhibition of mammalian lanosterol 14 alpha-demethylase: a possible strategy for cholesterol lowering. |
| AID262713 | Inhibition of human CYP3A4 | 2006 | Journal of medicinal chemistry, Apr-06, Volume: 49, Issue:7 | Synthesis and evaluation of heteroaryl-substituted dihydronaphthalenes and indenes: potent and selective inhibitors of aldosterone synthase (CYP11B2) for the treatment of congestive heart failure and myocardial fibrosis. |
| AID525141 | Antifungal activity against Fusarium moniliforme clade 3 by microdilution method | 2008 | Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6 | In vitro antifungal susceptibility and molecular characterization of clinical isolates of Fusarium verticillioides (F. moniliforme) and Fusarium thapsinum. |
| AID530960 | Antifungal activity against Candida tropicalis ATCC 750 after 48 hrs by CLSI method | 2008 | Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7 | Potent in vitro antifungal activities of naturally occurring acetylenic acids. |
| AID406958 | Antifungal activity against fluconazole-sensitive Candida albicans Fe40 at 35 degC after 48 hrs by broth microdilution test | 2008 | Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13 | 1-[(3-Aryloxy-3-aryl)propyl]-1H-imidazoles, new imidazoles with potent activity against Candida albicans and dermatophytes. Synthesis, structure-activity relationship, and molecular modeling studies. |
| AID402398 | Antifungal activity against Candida albicans SC5314 | 1998 | Journal of natural products, Oct, Volume: 61, Issue:10 | DNA-damaging steroidal alkaloids from Eclipta alba from the suriname rainforest1. |
| AID606215 | Antifungal activity against Cryptococcus neoformans ATCC BLS108 after 72 hrs by micro-broth dilution method | 2011 | European journal of medicinal chemistry, Jul, Volume: 46, Issue:7 | Design, synthesis and antifungal activities of novel 1,2,4-triazole derivatives. |
| AID406862 | Antimicrobial activity against Candida albicans GDH2346 at planktonic cell density of 10'3 cells/ml after 48 hrs by XTT assay | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | Role for cell density in antifungal drug resistance in Candida albicans biofilms. |
| AID391493 | Antifungal activity against Aspergillus niger ATCC 9029 after 48 hrs by spectrophotometry | 2008 | Journal of natural products, Oct, Volume: 71, Issue:10 | Evidence for the mechanism of action of the antifungal phytolaccoside B isolated from Phytolacca tetramera Hauman. |
| AID405016 | Antifungal activity against Sporothrix schenckii P25013 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by Sensititre YeastOne method | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods. |
| AID1110743 | Antifungal activity against Pichia kudriavzevii E 28 after 48 hr by microdilution broth method | 2002 | Farmaco (Societa chimica italiana : 1989), Feb, Volume: 57, Issue:2 | Ring substituted 3-phenyl-1-(2-pyrazinyl)-2-propen-1-ones as potential photosynthesis-inhibiting, antifungal and antimycobacterial agents. |
| AID282366 | Inhibition of ATRA hydroxylase in Syrian golden hamster liver microsome assessed ATRA metabolism using [11.12-3H]-ATRA | 2004 | Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27 | Novel retinoic acid metabolism blocking agents endowed with multiple biological activities are efficient growth inhibitors of human breast and prostate cancer cells in vitro and a human breast tumor xenograft in nude mice. |
| AID290145 | Antibacterial activity against Escherichia coli after 24 hrs by MTT colorimetric method | 2007 | European journal of medicinal chemistry, Apr, Volume: 42, Issue:4 | Synthesis and antimicrobial activities of Schiff bases derived from 5-chloro-salicylaldehyde. |
| AID530963 | Antifungal activity against Candida glabrata ATCC 90030 after 48 hrs by CLSI methodCandida glabrata | 2008 | Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7 | Potent in vitro antifungal activities of naturally occurring acetylenic acids. |
| AID1110741 | Antifungal activity against Candida glabrata 20/I after 24 hr by microdilution broth method | 2002 | Farmaco (Societa chimica italiana : 1989), Feb, Volume: 57, Issue:2 | Ring substituted 3-phenyl-1-(2-pyrazinyl)-2-propen-1-ones as potential photosynthesis-inhibiting, antifungal and antimycobacterial agents. |
| AID42885 | Inhibition of Candida parapsilosis ATCC 22019 growth for 48 hours in vitro. | 2001 | Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17 | 3-Phenyl-5-acyloxymethyl-2H,5H-furan-2-ones: synthesis and biological activity of a novel group of potential antifungal drugs. |
| AID481664 | Antifungal activity against Candida krusei NRRL Y-7179 after 24 hrs by broth microdilution assay | 2010 | European journal of medicinal chemistry, May, Volume: 45, Issue:5 | Synthesis and the selective antifungal activity of 5,6,7,8-tetrahydroimidazo[1,2-a]pyridine derivatives. |
| AID367157 | Antimicrobial activity against Candida albicans by broth microdilution method | 2009 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 19, Issue:3 | Synthesis and antifungal activity of 1,2,3-triazole containing fluconazole analogues. |
| AID1130382 | Antifungal activity against Saprolegnia Sp. assessed as growth inhibition in sabouraud broth after 14 days | 1979 | Journal of medicinal chemistry, Aug, Volume: 22, Issue:8 | Antimycotic imidazoles. part 4. Synthesis and antifungal activity of ketoconazole, a new potent orally active broad-spectrum antifungal agent. |
| AID49982 | Minimum inhibitory concentration of compound for antifungal activity against Candida glabrata | 2000 | Bioorganic & medicinal chemistry letters, Oct-02, Volume: 10, Issue:19 | Novel antifungals based on 4-substituted imidazole: a combinatorial chemistry approach to lead discovery and optimization. |
| AID1067043 | Antifungal activity against Trichophyton rubrum by micro-broth dilution method | 2014 | European journal of medicinal chemistry, Mar-03, Volume: 74 | Synthesis, antifungal activities and molecular docking studies of novel 2-(2,4-difluorophenyl)-2-hydroxy-3-(1H-1,2,4-triazol-1-yl)propyl dithiocarbamates. |
| AID426403 | Inhibition of recombinant CYP11B1 expressed in expressed in V79MZh11B1 cells at 2 uM | 2009 | European journal of medicinal chemistry, Jul, Volume: 44, Issue:7 | Novel CYP17 inhibitors: synthesis, biological evaluation, structure-activity relationships and modelling of methoxy- and hydroxy-substituted methyleneimidazolyl biphenyls. |
| AID395648 | Antifungal activity against Candida albicans ATCC 10231 assessed as growth inhibition at 50 uM after 24 hrs | 2009 | European journal of medicinal chemistry, Jan, Volume: 44, Issue:1 | Penetratin and derivatives acting as antifungal agents. |
| AID322753 | Inhibition of human CYP51 expressed in Topp 3 cells by lanosterol demethylase assay | 2007 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 35, Issue:3 | Three-dimensional quantitative structure-activity relationship analysis of human CYP51 inhibitors. |
| AID463563 | Inhibition of human recombinant aromatase at 10 uM | 2010 | Journal of natural products, Feb-26, Volume: 73, Issue:2 | The taiwaniaquinoids: a review. |
| AID666778 | Antibacterial activity against Escherichia coli at 0.05 mg by agar diffusion test | 2012 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 22, Issue:13 | Bioactive briarane diterpenoids from the South China Sea gorgonian Dichotella gemmacea. |
| AID524792 | Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR green assay | 2009 | Nature chemical biology, Oct, Volume: 5, Issue:10 | Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum. |
| AID555819 | Antifungal activity against cdr1/cdr1/cdr2/cdr2 deficient Candida albicans STY31 after 48 hrs | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | Relative contributions of the Candida albicans ABC transporters Cdr1p and Cdr2p to clinical azole resistance. |
| AID1067042 | Antifungal activity against Microsporum gypseum by micro-broth dilution method | 2014 | European journal of medicinal chemistry, Mar-03, Volume: 74 | Synthesis, antifungal activities and molecular docking studies of novel 2-(2,4-difluorophenyl)-2-hydroxy-3-(1H-1,2,4-triazol-1-yl)propyl dithiocarbamates. |
| AID334237 | Antimicrobial activity against Trichophyton tonsurans EQ 4329 after 10 days by microdilution technique | 2002 | Journal of natural products, Apr, Volume: 65, Issue:4 | Antimicrobial activities of a new schizozygane indoline alkaloid from Schizozygia coffaeoides and the revised structure of isoschizogaline. |
| AID1328089 | Antibacterial activity against Bacillus subtilis after 24 hrs by broth dilution method | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | Synthesis and antimicrobial activity of styryl/pyrrolyl/pyrazolyl sulfonylmethyl-1,3,4-oxadiazolyl amines and styryl/pyrrolyl/pyrazolyl sulfonylmethyl-1,3,4-thiadiazolyl amines. |
| AID608338 | Antifungal activity against 1 x 10'4 cfu/mL Candida albicans ATCC 6258 after 48 hrs by NCCLS M38-P microtiter broth dilution method | 2011 | European journal of medicinal chemistry, Aug, Volume: 46, Issue:8 | Synthesis and antimicrobial evaluation of new benzofuran derivatives. |
| AID362820 | Antifungal activity against Aspergillus niger after 48 hrs by microdilution susceptibility method | 2008 | European journal of medicinal chemistry, May, Volume: 43, Issue:5 | Synthesis and antimicrobial activity of novel sulfone-linked bis heterocycles. |
| AID555815 | Antifungal activity against tac1/tac1 deficient Candida albicans SZY31 after 48 hrs | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | Relative contributions of the Candida albicans ABC transporters Cdr1p and Cdr2p to clinical azole resistance. |
| AID667061 | Antifungal activity against Aspergillus niger after 48 hrs by broth dilution method | 2012 | European journal of medicinal chemistry, Aug, Volume: 54 | Synthesis, antimicrobial and cytotoxic activities of sulfone linked bis heterocycles. |
| AID287380 | Antifungal activity against Candida albicans after 24 hrs by disk diffusion method | 2007 | European journal of medicinal chemistry, Feb, Volume: 42, Issue:2 | Synthesis, characterization and antimicrobial activity of Fe(II), Zn(II), Cd(II) and Hg(II) complexes with 2,6-bis(benzimidazol-2-yl) pyridine ligand. |
| AID575118 | Antifungal activity against Madurella mycetomatis isolate 68 by XTT assay | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Madurella mycetomatis is not susceptible to the echinocandin class of antifungal agents. |
| AID490994 | Antifungal activity against sCurvularia lunata at 200 ug/disk after 48 hrs by disk diffusion method | 2010 | European journal of medicinal chemistry, Jul, Volume: 45, Issue:7 | Synthesis and bioassay of pyrrolyl oxazolines and thiazolines. |
| AID39834 | Minimum inhibitory concentration against Aspergillus fumigatus | 2004 | Bioorganic & medicinal chemistry letters, Jan-19, Volume: 14, Issue:2 | Synthesis of galactopyranosyl amino alcohols as a new class of antitubercular and antifungal agents. |
| AID1328454 | Selectivity ratio of IC50 for human Cyp3A4 to IC50 for recombinant CYP17 (unknown origin) overexpressed in human AD293 cells | 2016 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 26, Issue:23 | Design, synthesis, and evaluation of (2S,4R)-Ketoconazole sulfonamide analogs as potential treatments for Metabolic Syndrome. |
| AID432803 | Antifungal activity against Sporothrix albicans after 72 hrs by microdilution method | 2008 | Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2 | In vitro antifungal susceptibilities of five species of sporothrix. |
| AID1328090 | Antibacterial activity against Pseudomonas aeruginosa after 24 hrs by broth dilution method | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | Synthesis and antimicrobial activity of styryl/pyrrolyl/pyrazolyl sulfonylmethyl-1,3,4-oxadiazolyl amines and styryl/pyrrolyl/pyrazolyl sulfonylmethyl-1,3,4-thiadiazolyl amines. |
| AID1129361 | Unbound fraction in HEK293 cell homogenate at 0.1 uM by equilibrium dialysis based UPLC-MS/MS analysis | 2014 | Journal of medicinal chemistry, Apr-10, Volume: 57, Issue:7 | A high-throughput cell-based method to predict the unbound drug fraction in the brain. |
| AID1472624 | In vitro antifungal activity against Microsporum gypseum after 7 days by serial dilution method | 2018 | Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1 | Novel Terminal Bipheny-Based Diapophytoene Desaturases (CrtN) Inhibitors as Anti-MRSA/VISR/LRSA Agents with Reduced hERG Activity. |
| AID49123 | In vitro antifungal activity against 40 strains at pH 7.2 | 2002 | Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13 | Antifungal agents. 10. New derivatives of 1-[(aryl)[4-aryl-1H-pyrrol-3-yl]methyl]-1H-imidazole, synthesis, anti-candida activity, and quantitative structure-analysis relationship studies. |
| AID340961 | Antifungal activity against Candida albidus isolates from grapes by NCCLS M27-A2 method | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8 | Cross-resistance to medical and agricultural azole drugs in yeasts from the oropharynx of human immunodeficiency virus patients and from environmental Bavarian vine grapes. |
| AID596528 | Antifungal activity against Trichophyton rubrum C 113 2000 | 2011 | Bioorganic & medicinal chemistry, May-01, Volume: 19, Issue:9 | Antifungal, cytotoxic and SAR studies of a series of N-alkyl, N-aryl and N-alkylphenyl-1,4-pyrrolediones and related compounds. |
| AID29139 | Calculated dissociation constant (pKa, calculated with ACD/pKa) | 2002 | Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26 | Pharmacophore model of drugs involved in P-glycoprotein multidrug resistance: explanation of structural variety (hypothesis). |
| AID214278 | Minimum inhibitory concentration against Trichophyton mentagrophytes | 2004 | Bioorganic & medicinal chemistry letters, Jan-19, Volume: 14, Issue:2 | Synthesis of galactopyranosyl amino alcohols as a new class of antitubercular and antifungal agents. |
| AID680293 | TP_TRANSPORTER: increase in Calcein-AM intracellular accumulation (Calcein-AM: 0.5 uM, Ketoconazole: 50 uM) in MDR1-expressing NIH-3T3 cells | 2004 | Biochemical and biophysical research communications, Mar-19, Volume: 315, Issue:4 | Distinct groups of multidrug resistance modulating agents are distinguished by competition of P-glycoprotein-specific antibodies. |
| AID1222389 | Inhibition of human recombinant UGT1A1 expressed in HEK293 cells assessed as reduction in estradiol 3-glucuronidation by LC-MS/MS method | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2 | Correlation between bilirubin glucuronidation and estradiol-3-gluronidation in the presence of model UDP-glucuronosyltransferase 1A1 substrates/inhibitors. |
| AID214279 | Minimum inhibitory concentration of compound for antifungal activity against Trichophyton mentagrophytes | 2000 | Bioorganic & medicinal chemistry letters, Oct-02, Volume: 10, Issue:19 | Novel antifungals based on 4-substituted imidazole: a combinatorial chemistry approach to lead discovery and optimization. |
| AID574060 | Antifungal activity against 10'3 cells/ml wild-type Candida albicans BF-1 by NCCLS method | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | Cell density and cell aging as factors modulating antifungal resistance of Candida albicans biofilms. |
| AID150753 | Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay | 2003 | Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9 | Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery. |
| AID521220 | Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay | 2007 | Nature chemical biology, May, Volume: 3, Issue:5 | Chemical genetics reveals a complex functional ground state of neural stem cells. |
| AID616875 | Antimicrobial activity against Pseudomonas aeruginosa after 24 hrs by agar dilution method | 2011 | Journal of natural products, Aug-26, Volume: 74, Issue:8 | Cytotoxic bipyridines from the marine-derived actinomycete Actinoalloteichus cyanogriseus WH1-2216-6. |
| AID150618 | Concentration required for 50% inhibition at binding site of human P-Glycoprotein (P-gp) in one-affinity model | 2002 | Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26 | Pharmacophore model of drugs involved in P-glycoprotein multidrug resistance: explanation of structural variety (hypothesis). |
| AID1210016 | Inhibition of CYP2C8 in human liver microsomes using paclitaxel as substrate after 8 mins by LC-MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5 | Identifying a selective substrate and inhibitor pair for the evaluation of CYP2J2 activity. |
| AID482322 | Inhibition of human CYP17 expressed in Escherichia coli | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Novel highly potent and selective nonsteroidal aromatase inhibitors: synthesis, biological evaluation and structure-activity relationships investigation. |
| AID363743 | Antimicrobial activity against Cryptococcus neoformans IM 972724 isolate at 6.25 ug/ml after 48 hrs | 2008 | Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17 | In vitro antifungal activity of polyfunctionalized 2-(hetero)arylquinolines prepared through imino Diels-Alder reactions. |
| AID623353 | Antifungal activity against Candida albicans clinical isolate by NCCLS M27-A2 microbroth dilution method | 2011 | European journal of medicinal chemistry, Nov, Volume: 46, Issue:11 | Synthesis and anticandidal activity of new triazolothiadiazine derivatives. |
| AID486238 | Antifungal activity against Aspergillus fumigatus ATCC 26934 after 48 hrs | 2010 | European journal of medicinal chemistry, Jun, Volume: 45, Issue:6 | Naftifine-analogues as anti-Trypanosoma cruzi agents. |
| AID322161 | Antifungal activity against Candida lusitaniae C 131-2000 after 48 hrs by CLSI M27-A2 method | 2008 | Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1 | N-Phenyl and N-phenylalkyl-maleimides acting against Candida spp.: time-to-kill, stability, interaction with maleamic acids. |
| AID1110734 | Antifungal activity against Lichtheimia corymbifera 272 after 24 hr by microdilution broth method | 2002 | Farmaco (Societa chimica italiana : 1989), Feb, Volume: 57, Issue:2 | Ring substituted 3-phenyl-1-(2-pyrazinyl)-2-propen-1-ones as potential photosynthesis-inhibiting, antifungal and antimycobacterial agents. |
| AID1300878 | Antifungal activity against Candida albicans clinical isolate after 24 hrs by broth microdilution method | 2016 | European journal of medicinal chemistry, Jul-19, Volume: 117 | Novel 1,3-thiazolidin-4-one derivatives as promising anti-Candida agents endowed with anti-oxidant and chelating properties. |
| AID432801 | Antifungal activity against Sporothrix globosa after 72 hrs by microdilution method | 2008 | Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2 | In vitro antifungal susceptibilities of five species of sporothrix. |
| AID572709 | Selectivity ratio of Kd for Mycobacterium smegmatis ATCC 700084 CYP164A2 in presence of 0.5 M NaCl to Kd for Mycobacterium smegmatis ATCC 700084 CYP164A2 | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | Identification, characterization, and azole-binding properties of Mycobacterium smegmatis CYP164A2, a homolog of ML2088, the sole cytochrome P450 gene of Mycobacterium leprae. |
| AID287720 | Inhibition of human recombinant aromatase at 300 nM after 30 mins relative to control | 2007 | Bioorganic & medicinal chemistry, Apr-01, Volume: 15, Issue:7 | Synthesis of DL-standishinal and its related compounds for the studies on structure-activity relationship of inhibitory activity against aromatase. |
| AID322159 | Antifungal activity against Candida glabrata C 115-2000 after 48 hrs by CLSI M27-A2 method | 2008 | Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1 | N-Phenyl and N-phenylalkyl-maleimides acting against Candida spp.: time-to-kill, stability, interaction with maleamic acids. |
| AID303378 | Antitrypanosomal activity against Trypanosoma cruzi Tulahuen 2 | 2007 | Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24 | In vivo anti-Chagas vinylthio-, vinylsulfinyl-, and vinylsulfonylbenzofuroxan derivatives. |
| AID241455 | Inhibitory activity against 25-hydroxyvitamin D3 24-hydroxylase of rat kidney mitochondria | 2004 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 14, Issue:22 | Synthesis and CYP24 inhibitory activity of 2-substituted-3,4-dihydro-2H-naphthalen-1-one (tetralone) derivatives. |
| AID49461 | Antifungal activity in rat vaginal candidasis, 3 day postinfection with Candida. albicans SOB FM-391 | 1988 | Journal of medicinal chemistry, Oct, Volume: 31, Issue:10 | Studies on antifungal agents. 23. Novel substituted 3,5-diphenyl-3-(1H-imidazol-1-ylmethyl)- 2-alkylisoxazolidine derivatives. |
| AID596526 | Antifungal activity against Aspergillus niger ATCC 9029 | 2011 | Bioorganic & medicinal chemistry, May-01, Volume: 19, Issue:9 | Antifungal, cytotoxic and SAR studies of a series of N-alkyl, N-aryl and N-alkylphenyl-1,4-pyrrolediones and related compounds. |
| AID406954 | Cytotoxicity against human K562 cells after assessed as reduction of cell viability 24 hrs by MTT assay | 2008 | Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13 | 1-[(3-Aryloxy-3-aryl)propyl]-1H-imidazoles, new imidazoles with potent activity against Candida albicans and dermatophytes. Synthesis, structure-activity relationship, and molecular modeling studies. |
| AID1104301 | Antifungal activity against Aspergillus versicolor ATCC 11730 at 28 degC measured after 72 hr by microdilution method | 2010 | Chemical & pharmaceutical bulletin, Feb, Volume: 58, Issue:2 | Sulfonamide-1,2,4-thiadiazole derivatives as antifungal and antibacterial agents: synthesis, biological evaluation, lipophilicity, and conformational studies. |
| AID481915 | Antifungal activity against Candida krusei ATCC 27803 at 15 ug in 6 mm after 10 hrs by disc-diffusion assay | 2010 | Journal of natural products, May-28, Volume: 73, Issue:5 | Chemical epigenetics alters the secondary metabolite composition of guttate excreted by an atlantic-forest-soil-derived Penicillium citreonigrum. |
| AID564266 | Effect on sterol composition in Candida albicans isolate 108 harboring erg11 and erg5 double mutant assessed as obtusifoliol level after 2 hrs by gas chromatography | 2010 | Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9 | A clinical isolate of Candida albicans with mutations in ERG11 (encoding sterol 14alpha-demethylase) and ERG5 (encoding C22 desaturase) is cross resistant to azoles and amphotericin B. |
| AID49113 | In vitro antifungal activity against 40 strains at pH 7.2 | 2002 | Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13 | Antifungal agents. 10. New derivatives of 1-[(aryl)[4-aryl-1H-pyrrol-3-yl]methyl]-1H-imidazole, synthesis, anti-candida activity, and quantitative structure-analysis relationship studies. |
| AID530962 | Antifungal activity against Candida krusei ATCC 6258 after 48 hrs by CLSI method | 2008 | Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7 | Potent in vitro antifungal activities of naturally occurring acetylenic acids. |
| AID1104303 | Antifungal activity against Aspergillus niger ATCC 6275 at 28 degC measured after 72 hr by microdilution method | 2010 | Chemical & pharmaceutical bulletin, Feb, Volume: 58, Issue:2 | Sulfonamide-1,2,4-thiadiazole derivatives as antifungal and antibacterial agents: synthesis, biological evaluation, lipophilicity, and conformational studies. |
| AID48751 | Minimum inhibitory concentration against Candida albicans ATCC 10231 | 2004 | Bioorganic & medicinal chemistry letters, Feb-09, Volume: 14, Issue:3 | Synthesis and antifungal activities of phenylenedithioureas. |
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| AID406952 | Antifungal activity against Candida albicans ATCC 10261 at 35 degC after 48 to 96 hrs by broth microdilution test | 2008 | Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13 | 1-[(3-Aryloxy-3-aryl)propyl]-1H-imidazoles, new imidazoles with potent activity against Candida albicans and dermatophytes. Synthesis, structure-activity relationship, and molecular modeling studies. |
| AID422129 | Antimicrobial activity against Candida albicans by broth microdilution assay | 2009 | Journal of natural products, May-22, Volume: 72, Issue:5 | Antimicrobial ambiguine isonitriles from the cyanobacterium Fischerella ambigua. |
| AID362916 | Antifungal activity against Aspergillus terreus after 24 hrs by broth microdilution method | 2008 | Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17 | NO-donors. Part 17: Synthesis and antimicrobial activity of novel ketoconazole-NO-donor hybrid compounds. |
| AID334238 | Antimicrobial activity against Trichophyton interdigitale EQ 4115 after 10 days by microdilution technique | 2002 | Journal of natural products, Apr, Volume: 65, Issue:4 | Antimicrobial activities of a new schizozygane indoline alkaloid from Schizozygia coffaeoides and the revised structure of isoschizogaline. |
| AID1263197 | Inhibition of human prostate type 2 5alpha-reductase assessed as transformation of testosterone to dihydrotestosterone | 2015 | Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24 | Synthesis and activity of novel 16-dehydropregnenolone acetate derivatives as inhibitors of type 1 5α-reductase and on cancer cell line SK-LU-1. |
| AID376052 | Antifungal activity against Aspergillus flavus ATCC 9170 by agar dilution method | 1999 | Journal of natural products, Oct, Volume: 62, Issue:10 | In vitro evaluation of antifungal properties of phenylpropanoids and related compounds acting against dermatophytes. |
| AID625290 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID1157292 | Antifungal activity against Candida parapsilosis 22019 assessed as growth inhibition by automatic microplate reader analysis | 2014 | Journal of natural products, May-23, Volume: 77, Issue:5 | Polyhydroxy cyclohexanols from a Dendrodochium sp. fungus associated with the sea cucumber Holothuria nobilis Selenka. |
| AID696538 | Antifungal activity against Saccharomyces cerevisiae ATCC 9763 after 48 hrs by broth microdilution technique | 2012 | Bioorganic & medicinal chemistry, Nov-01, Volume: 20, Issue:21 | Synthesis and antifungal activity of diverse C-2 pyridinyl and pyridinylvinyl substituted quinolines. |
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| AID141784 | In vitro antifungal activity against Mucor sp | 1984 | Journal of medicinal chemistry, Jul, Volume: 27, Issue:7 | Antimycotic azoles. 7. Synthesis and antifungal properties of a series of novel triazol-3-ones. |
| AID563611 | Effect on sterol composition in Candida albicans isolate 108 harboring erg11 and erg5 double mutant assessed as ergosta 5,7-dienol level after 2 hrs by gas chromatography | 2010 | Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9 | A clinical isolate of Candida albicans with mutations in ERG11 (encoding sterol 14alpha-demethylase) and ERG5 (encoding C22 desaturase) is cross resistant to azoles and amphotericin B. |
| AID405010 | Antifungal activity against Sporothrix schenckii P0019 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by Sensititre YeastOne method | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods. |
| AID477743 | Antimicrobial activity against Cryptococcus neoformans after 24 hrs | 2010 | European journal of medicinal chemistry, Apr, Volume: 45, Issue:4 | An eco-friendly synthesis and antimicrobial activities of dihydro-2H-benzo- and naphtho-1,3-oxazine derivatives. |
| AID624629 | Inhibition of Pgp expressed in MDR1-MDCKII cells measured by calcein-AM assay | 2001 | The Journal of pharmacology and experimental therapeutics, Nov, Volume: 299, Issue:2 | Rational use of in vitro P-glycoprotein assays in drug discovery. |
| AID227889 | In vivo activity against microsporosis guinea pig, measured as the ratio of animals cured/animals infected (C/I) at dose 10 mg/kg; 4/34 | 1984 | Journal of medicinal chemistry, Jul, Volume: 27, Issue:7 | Antimycotic azoles. 7. Synthesis and antifungal properties of a series of novel triazol-3-ones. |
| AID575119 | Antifungal activity against Madurella mycetomatis isolate 73 by XTT assay | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Madurella mycetomatis is not susceptible to the echinocandin class of antifungal agents. |
| AID377676 | Antifungal activity against Candida shehatae after 48 hrs by NCCLS M27A method | 2006 | Journal of natural products, Jul, Volume: 69, Issue:7 | Phytochemistry and antifungal properties of the newly discovered tree Pleodendron costaricense. |
| AID420065 | Antifungal activity against Candida albicans PCA-2 after 48 hrs by broth microdilution assay | 2009 | Bioorganic & medicinal chemistry, Jun-01, Volume: 17, Issue:11 | Bulky 1,4-benzoxazine derivatives with antifungal activity. |
| AID1155711 | Antifungal activity against Aspergillus niger assessed as growth inhibition after 48 hrs by broth dilution method | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Synthesis and antimicrobial activity of amine linked bis- and tris-heterocycles. |
| AID130720 | In vivo inhibitory activity against phorbol myristyl acetate (PMA) ear edema at a dose of 100 ug/ear | 1992 | Journal of medicinal chemistry, Aug-21, Volume: 35, Issue:17 | Novel 1-(pyridylphenyl)-1-phenyl-2-imidazolylethanols with topical antiinflammatory activity. |
| AID341764 | Cmax in human plasma at 200 mg qd for 4 days | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8 | Fosamprenavir plus ritonavir increases plasma ketoconazole and ritonavir exposure, while amprenavir exposure remains unchanged. |
| AID1184072 | Cytotoxicity against mouse P815B cells after 24 hrs by MTS/PMS assay | 2014 | European journal of medicinal chemistry, Sep-12, Volume: 84 | Detailed analysis and follow-up studies of a high-throughput screening for indoleamine 2,3-dioxygenase 1 (IDO1) inhibitors. |
| AID753830 | Antimicrobial activity against Candida albicans SC5314 | 2013 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 23, Issue:12 | 3-Anhydro-6-hydroxy-ophiobolin A, a new sesterterpene inhibiting the growth of methicillin-resistant Staphylococcus aureus and inducing the cell death by apoptosis on K562, from the phytopathogenic fungus Bipolaris oryzae. |
| AID648382 | Antifungal activity against Candida albicans MTCC 227 after 48 to 72 hrs by twofold serial dilution method | 2012 | European journal of medicinal chemistry, May, Volume: 51 | Synthesis of novel spirooxindole derivatives by one pot multicomponent reaction and their antimicrobial activity. |
| AID637041 | Antifungal activity against Candida albicans at 100 ug/disc after 24 hrs by disc diffusion method | 2012 | European journal of medicinal chemistry, Feb, Volume: 48 | Synthesis and biological evaluation of some thiazolidinones as antimicrobial agents. |
| AID407013 | Antimicrobial activity against Cdr1, Cdr2 and Mdr1 deficient Candida albicans DSY1050 at planktonic cell density of 10'3 cells/ml after 48 hrs by XTT assay | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | Role for cell density in antifungal drug resistance in Candida albicans biofilms. |
| AID49462 | Antifungal activity in rat vaginal candidasis, 4 day postinfection with Candida. albicans SOB FM-391 | 1988 | Journal of medicinal chemistry, Oct, Volume: 31, Issue:10 | Studies on antifungal agents. 23. Novel substituted 3,5-diphenyl-3-(1H-imidazol-1-ylmethyl)- 2-alkylisoxazolidine derivatives. |
| AID330525 | Antifungal activity against Candida parapsilosis infected cyclophosphamide-immunocompromized Crl:CD1(ICR) mouse assessed as fungal density in kidney at 0.5 mg/kg, po for 5 days measured on day 12 | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Mar-13, Volume: 104, Issue:11 | High-throughput synergy screening identifies microbial metabolites as combination agents for the treatment of fungal infections. |
| AID42857 | Inhibition of Candida albicans ATCC 90028 for 24 hours in vitro. | 2001 | Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17 | 3-Phenyl-5-acyloxymethyl-2H,5H-furan-2-ones: synthesis and biological activity of a novel group of potential antifungal drugs. |
| AID628512 | Antifungal activity against Candida albicans at 200 ug/ml after 48 hrs by disc diffusion method | 2011 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21 | Synthesis and biological evaluation of some novel triazol-3-ones as antimicrobial agents. |
| AID1179288 | Antimicrobial activity against Candida albicans MTCC 227 after 48 to 72 hrs by two fold dilution method | 2014 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 24, Issue:14 | Synthesis, antimicrobial and molecular docking studies of enantiomerically pure N-alkylated β-amino alcohols from phenylpropanolamines. |
| AID348962 | Antifungal activity against Aspergillus niger after 48 hrs by MTT assay | 2008 | European journal of medicinal chemistry, Jul, Volume: 43, Issue:7 | Synthesis and antimicrobial activities of 7-O-modified genistein derivatives. |
| AID531205 | Antifungal activity against Candida albicans ATCC 14053 after 48 hrs by CLSI method | 2008 | Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7 | Potent in vitro antifungal activities of naturally occurring acetylenic acids. |
| AID1332942 | Antifungal activity against Aspergillus niger MTCC 1881 at 200 ug/mL incubated at 4 degC for 24 hrs followed by subsequent incubation at 37.5 degC for 3 days by poisoned food method | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Synthesis, antimicrobial activity and advances in structure-activity relationships (SARs) of novel tri-substituted thiazole derivatives. |
| AID1130387 | Antifungal activity against Microsporum canis assessed as growth inhibition in sabouraud broth after 14 days in presence of 10% inactivated bovine serum | 1979 | Journal of medicinal chemistry, Aug, Volume: 22, Issue:8 | Antimycotic imidazoles. part 4. Synthesis and antifungal activity of ketoconazole, a new potent orally active broad-spectrum antifungal agent. |
| AID218573 | Effect of increase in enzyme concentration by 10 times on the inhibition of beta-lactamase by the compound:No inhibition | 2003 | Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21 | Identification and prediction of promiscuous aggregating inhibitors among known drugs. |
| AID532547 | Antifungal activity against wild-type Saccharomyces cerevisiae BY4741 assessed as accumulation of ergosterol at 4 ug/ml (Rvb = 57+/- 1.00 %) | 2008 | Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10 | Differential azole antifungal efficacies contrasted using a Saccharomyces cerevisiae strain humanized for sterol 14 alpha-demethylase at the homologous locus. |
| AID625287 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID456687 | Antifungal activity against Cryptococcus neoformans ATCC 32264 assessed as inhibition of fungal growth at 3.125 uM after 48 hrs by microbroth dilution method | 2010 | Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1 | New small-size peptides possessing antifungal activity. |
| AID325038 | Antimicrobial activity against Candida albicans P5 after 48 hrs by broth macrodilution method | 2007 | Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5 | A Candida albicans petite mutant strain with uncoupled oxidative phosphorylation overexpresses MDR1 and has diminished susceptibility to fluconazole and voriconazole. |
| AID49131 | Tested for minimum subinhibitory concentration against Candida albicans 124 (Candida albicans) at pH 6.5. | 1994 | Journal of medicinal chemistry, Jun-24, Volume: 37, Issue:13 | Derivatives of a novel cyclopeptolide. 1. Synthesis, antifungal activity, and structure-activity relationships. |
| AID648372 | Antifungal activity against Botrytis cinerea at 1000 ug/disc after 48 hrs by disc diffusion assay | 2012 | European journal of medicinal chemistry, May, Volume: 51 | Synthesis of novel spirooxindole derivatives by one pot multicomponent reaction and their antimicrobial activity. |
| AID654682 | Inhibition of human recombinant aromatase expressed in baculovirus/insect cells using 7-methoxy-trifluoromethylcoumarin as substrate after 30 mins by fluorescence-based spectrophotometry | 2012 | Bioorganic & medicinal chemistry, Apr-15, Volume: 20, Issue:8 | Development of a new class of aromatase inhibitors: design, synthesis and inhibitory activity of 3-phenylchroman-4-one (isoflavanone) derivatives. |
| AID284089 | Antifungal activity against Candida albicans C128-2000 after 48 hrs | 2007 | Bioorganic & medicinal chemistry, Jan-01, Volume: 15, Issue:1 | Synthesis and antifungal activity of (Z)-5-arylidenerhodanines. |
| AID284093 | Antifungal activity against Candida parapsilosis C124-2000 after 48 hrs | 2007 | Bioorganic & medicinal chemistry, Jan-01, Volume: 15, Issue:1 | Synthesis and antifungal activity of (Z)-5-arylidenerhodanines. |
| AID530958 | Antifungal activity against Cryptococcus neoformans ATCC 66031 after 72 hrs by CLSI method | 2008 | Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7 | Potent in vitro antifungal activities of naturally occurring acetylenic acids. |
| AID406959 | Antifungal activity against dermatophytes at 28 degC after 7 days by broth microdilution test | 2008 | Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13 | 1-[(3-Aryloxy-3-aryl)propyl]-1H-imidazoles, new imidazoles with potent activity against Candida albicans and dermatophytes. Synthesis, structure-activity relationship, and molecular modeling studies. |
| AID575113 | Antifungal activity against Madurella mycetomatis isolate 50 by XTT assay | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Madurella mycetomatis is not susceptible to the echinocandin class of antifungal agents. |
| AID633995 | Antifungal activity against Saccharomyces cerevisiae ATCC 24657 assessed as growth inhibition at 31.2 uM after 24 to 48 hrs by spectrophotometric bioassay | 2012 | European journal of medicinal chemistry, Jan, Volume: 47, Issue:1 | Antifungal activities of novel non-azole molecules against S. cerevisiae and C. albicans. |
| AID492341 | Inhibition of human CYP24A1 expressed in chinese hamster V79 cells | 2010 | Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14 | Synthesis and CYP24A1 inhibitory activity of N-(2-(1H-imidazol-1-yl)-2-phenylethyl)arylamides. |
| AID511050 | Antimicrobial activity against Aspergillus niger NCIM 596 after 48 hrs by microdilution susceptibility method | 2010 | European journal of medicinal chemistry, Sep, Volume: 45, Issue:9 | Synthesis and bioassay of aminosulfonyl-1,3,4-oxadiazoles and their interconversion to 1,3,4-thiadiazoles. |
| AID381183 | Antifungal activity against Candida glabrata after 24 to 72 hrs by disk diffusion method | 1999 | Journal of natural products, Sep, Volume: 62, Issue:9 | Antimicrobial and antitumor activities of mycosporulone. |
| AID1328451 | Inhibition of recombinant CYP21 (unknown origin) overexpressed in human AD293 cells assessed as reduction in 11-deoxycortisol formation preincubated for 60 mins followed by addition of 17-alpha-hydroxyprogesterone as substrate measured after 45 mins by LC | 2016 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 26, Issue:23 | Design, synthesis, and evaluation of (2S,4R)-Ketoconazole sulfonamide analogs as potential treatments for Metabolic Syndrome. |
| AID407015 | Antimicrobial activity against Cdr1, Cdr2 and Mdr1 deficient Candida albicans DSY1050 dissociated biofilms at cell density of 10'3 cells/ml after 48 hrs by XTT assay | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | Role for cell density in antifungal drug resistance in Candida albicans biofilms. |
| AID1451793 | Antifungal activity against Microsporum gypseum after 7 days | 2017 | Journal of medicinal chemistry, 10-12, Volume: 60, Issue:19 | Novel Inhibitors of Staphyloxanthin Virulence Factor in Comparison with Linezolid and Vancomycin versus Methicillin-Resistant, Linezolid-Resistant, and Vancomycin-Intermediate Staphylococcus aureus Infections in Vivo. |
| AID1301005 | Inhibition of human recombinant CYP2C9 using MFC as substrate incubated for 40 mins by fluorimetry | 2016 | European journal of medicinal chemistry, Jul-19, Volume: 117 | 2-hydroxyisoquinoline-1,3(2H,4H)-diones (HIDs) as human immunodeficiency virus type 1 integrase inhibitors: Influence of the alkylcarboxamide substitution of position 4. |
| AID47892 | In vitro evaluation of minimum inhibitory concentration against Candida parapsilosis 61 | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20 | Synthesis and antifungal activity of new azole derivatives containing an N-acylmorpholine ring. |
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| AID48449 | In vitro antifungal activity against candida Spp (Candida glabrata, Candida krusei) at pH 5.8,(percent of resistant species at 256 ug/mL) | 2002 | Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13 | Antifungal agents. 10. New derivatives of 1-[(aryl)[4-aryl-1H-pyrrol-3-yl]methyl]-1H-imidazole, synthesis, anti-candida activity, and quantitative structure-analysis relationship studies. |
| AID638445 | Inhibition of human recombinant aromatase assessed as conversion of O-dibenzylfluorescein benzyl ester substrate to fluorescein byproduct by fluorometric assay | 2012 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1 | Discovery of a novel class of aldol-derived 1,2,3-triazoles: potent and selective inhibitors of human cytochrome P450 19A1 (aromatase). |
| AID655582 | Antifungal activity against Cryptococcus neoformans after 72 hrs by microbroth dilution method | 2012 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8 | New triazole derivatives as antifungal agents: synthesis via click reaction, in vitro evaluation and molecular docking studies. |
| AID1319266 | Inhibition of CYP3A4 in human liver microsomes using midazolam as substrate assessed as reduction in 4-OH-midazolam formation at 0.04 uM by LC/MS/MS analysis | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18 | Identification of (R)-(2-Chloro-3-(trifluoromethyl)phenyl)(1-(5-fluoropyridin-2-yl)-4-methyl-6,7-dihydro-1H-imidazo[4,5-c]pyridin-5(4H)-yl)methanone (JNJ 54166060), a Small Molecule Antagonist of the P2X7 receptor. |
| AID1129514 | Antimicrobial activity against Escherichia coli ATCC 25922 after 24 hrs by broth dilution method | 2014 | European journal of medicinal chemistry, Apr-22, Volume: 77 | Synthesis, antimicrobial and cytotoxic activities of pyrimidinyl benzoxazole, benzothiazole and benzimidazole. |
| AID530934 | Antifungal activity against Candida glabrata ATCC 90030 at 9.4 uM after 48 hrs by CLSI method | 2008 | Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7 | Potent in vitro antifungal activities of naturally occurring acetylenic acids. |
| AID633916 | Antifungal activity against Aspergillus niger ATCC 16404 by twofold serial dilution technique | 2012 | European journal of medicinal chemistry, Jan, Volume: 47, Issue:1 | Isoxazoles incorporated N-substituted decahydroquinolines: a precursor to the next generation antimicrobial drug. |
| AID45507 | Inhibitory activity against Candida albicans (40 clinical isolates), determined at pH-5.8 | 1995 | Journal of medicinal chemistry, Oct-13, Volume: 38, Issue:21 | Antifungal agents. 9. 3-Aryl-4-[alpha-(1H-imidazol-1-yl)arylmethyl]pyrroles: a new class of potent anti-Candida agents. |
| AID481670 | Cytotoxicity against human BT549 cells up to 25 ug/ml after 48 hrs by neutral red assay | 2010 | European journal of medicinal chemistry, May, Volume: 45, Issue:5 | Synthesis and the selective antifungal activity of 5,6,7,8-tetrahydroimidazo[1,2-a]pyridine derivatives. |
| AID290146 | Antibacterial activity against Pseudomonas fluorescens after 24 hrs by MTT colorimetric method | 2007 | European journal of medicinal chemistry, Apr, Volume: 42, Issue:4 | Synthesis and antimicrobial activities of Schiff bases derived from 5-chloro-salicylaldehyde. |
| AID481662 | Antifungal activity against Candida utilis NRRL Y-900 after 24 hrs by broth microdilution assay | 2010 | European journal of medicinal chemistry, May, Volume: 45, Issue:5 | Synthesis and the selective antifungal activity of 5,6,7,8-tetrahydroimidazo[1,2-a]pyridine derivatives. |
| AID717029 | Antifungal activity against Candida glabrata Anadolu University clinical isolate after 24 hrs by microdilution susceptibility assay | 2012 | European journal of medicinal chemistry, Dec, Volume: 58 | Synthesis and biological evaluation of some hydrazone derivatives as new anticandidal and anticancer agents. |
| AID481660 | Antifungal activity against Candida albicans ATCC 90028 after 24 hrs by broth microdilution assay | 2010 | European journal of medicinal chemistry, May, Volume: 45, Issue:5 | Synthesis and the selective antifungal activity of 5,6,7,8-tetrahydroimidazo[1,2-a]pyridine derivatives. |
| AID363749 | Antimicrobial activity against Candida albicans C130 isolate at 6.25 ug/ml after 24 hrs | 2008 | Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17 | In vitro antifungal activity of polyfunctionalized 2-(hetero)arylquinolines prepared through imino Diels-Alder reactions. |
| AID204352 | Minimum inhibitory concentration of compound for antifungal activity against Sporothrix schenck ii | 2000 | Bioorganic & medicinal chemistry letters, Oct-02, Volume: 10, Issue:19 | Novel antifungals based on 4-substituted imidazole: a combinatorial chemistry approach to lead discovery and optimization. |
| AID396968 | Antifungal activity against Curvularia lunata NCIM 716 after 48 hrs by microdilution susceptibility method | 2009 | European journal of medicinal chemistry, May, Volume: 44, Issue:5 | Synthesis, antimicrobial and cytotoxic activities of 1,3,4-oxadiazoles, 1,3,4-thiadiazoles and 1,2,4-triazoles. |
| AID588219 | FDA HLAED, gamma-glutamyl transferase (GGT) increase | 2004 | Current drug discovery technologies, Dec, Volume: 1, Issue:4 | Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling. |
| AID367160 | Antimicrobial activity against Trichophyton mentagrophytes by broth microdilution method | 2009 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 19, Issue:3 | Synthesis and antifungal activity of 1,2,3-triazole containing fluconazole analogues. |
| AID566956 | Antifungal activity against Cryptococcus neoformans ATCC 32264 assessed as inhibition of fungal growth at 25 uM after 48 hrs by microplate analysis | 2011 | European journal of medicinal chemistry, Jan, Volume: 46, Issue:1 | Penetratin analogues acting as antifungal agents. |
| AID774657 | Antitrypanosomal activity against amastigote stage of Trypanosoma cruzi infected in mouse NIH/3T3 cells after 48 hrs by Hoechst staining assay | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20 | Approaches to protozoan drug discovery: phenotypic screening. |
| AID207139 | Inhibition of human testicular steroid 17-alpha-hydroxylase | 1996 | Journal of medicinal chemistry, Oct-11, Volume: 39, Issue:21 | Synthesis and evaluation of pregnane derivatives as inhibitors of human testicular 17 alpha-hydroxylase/C17,20-lyase. |
| AID330523 | Antifungal activity against Candida parapsilosis infected cyclophosphamide-immunocompromized Crl:CD1(ICR) mouse assessed as survival at 10 mg/kg, po for 5 days | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Mar-13, Volume: 104, Issue:11 | High-throughput synergy screening identifies microbial metabolites as combination agents for the treatment of fungal infections. |
| AID625281 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID1328078 | Antifungal activity against Aspergillus niger assessed as inhibition of spore germination at 12.5 ug/well after 48 hrs by agar well diffusion method | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | Synthesis and antimicrobial activity of styryl/pyrrolyl/pyrazolyl sulfonylmethyl-1,3,4-oxadiazolyl amines and styryl/pyrrolyl/pyrazolyl sulfonylmethyl-1,3,4-thiadiazolyl amines. |
| AID372243 | Fungistatic activity against Candida albicans CHK21 after 24 to 48 hrs by broth microdilution assay | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10 | The Ssk1p response regulator and Chk1p histidine kinase mutants of Candida albicans are hypersensitive to fluconazole and voriconazole. |
| AID1168289 | Inhibition of CYP3A4 (unknown origin) using AMMC by fluorescence assay | 2014 | Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21 | Chemical synthesis, cytotoxicity, selectivity and bioavailability of 5α-androstane-3α,17β-diol derivatives. |
| AID343558 | Antitrypanosomal activity against epimastigotes of Trypanosoma cruzi CL Brener | 2008 | Bioorganic & medicinal chemistry, Jul-15, Volume: 16, Issue:14 | New trypanocidal hybrid compounds from the association of hydrazone moieties and benzofuroxan heterocycle. |
| AID141790 | Minimum inhibitory concentration of compound for antifungal activity against Mucosporam canis | 2000 | Bioorganic & medicinal chemistry letters, Oct-02, Volume: 10, Issue:19 | Novel antifungals based on 4-substituted imidazole: a combinatorial chemistry approach to lead discovery and optimization. |
| AID179678 | Tested for efficacy of compound in experimental vaginal candidosis (rat) after oral treatment at dosage of 2x 300 mg kg e-1 | 1994 | Journal of medicinal chemistry, Jun-24, Volume: 37, Issue:13 | Derivatives of a novel cyclopeptolide. 1. Synthesis, antifungal activity, and structure-activity relationships. |
| AID1152147 | Inhibition of recombinant CYP3A4 (unknown origin) using 7-benzyloxy-4-trifluoromethylcoumarin as substrate | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11 | Investigation of a novel series of 2-hydroxyisoquinoline-1,3(2H,4H)-diones as human immunodeficiency virus type 1 integrase inhibitors. |
| AID302124 | Antifungal activity against fluconazole-resistant Candida albicans 18 after 24 hrs | 2007 | Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22 | Synthesis and antifungal activities of novel 2-aminotetralin derivatives. |
| AID50127 | Evaluation of In vitro antifungal activity against Candida guilliermondii 26 by broth macro dilution method | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20 | Synthesis and antifungal activity of new azole derivatives containing an N-acylmorpholine ring. |
| AID428564 | Inhibition of CYP3A4 | 2009 | European journal of medicinal chemistry, Jul, Volume: 44, Issue:7 | Comparative chemometric modeling of cytochrome 3A4 inhibitory activity of structurally diverse compounds using stepwise MLR, FA-MLR, PLS, GFA, G/PLS and ANN techniques. |
| AID678715 | Inhibition of human CYP2D6 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 4-methylaminoethyl-7-methoxycoumarin as substrate after 30 mins | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
| AID405076 | Antifungal activity against Sporothrix schenckii isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by Sensititre YeastOne method | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods. |
| AID262556 | Antifungal activity against Microsporum lanosum | 2006 | Journal of medicinal chemistry, Apr-20, Volume: 49, Issue:8 | Structure-based optimization of azole antifungal agents by CoMFA, CoMSIA, and molecular docking. |
| AID494000 | Antifungal activity against Candida albicans ATCC 10231 assessed as inhibition of fungal growth at 25 uM | 2010 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 20, Issue:16 | New antifungal peptides. Synthesis, bioassays and initial structure prediction by CD spectroscopy. |
| AID564268 | Effect on sterol composition in Candida albicans isolate 108 harboring erg11 and erg5 double mutant eburicol level after 2 hrs by gas chromatography | 2010 | Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9 | A clinical isolate of Candida albicans with mutations in ERG11 (encoding sterol 14alpha-demethylase) and ERG5 (encoding C22 desaturase) is cross resistant to azoles and amphotericin B. |
| AID488643 | Antimicrobial activity against Candida dubliniensis ATCC 777 by broth dilution method | 2010 | Journal of natural products, Jun-25, Volume: 73, Issue:6 | Alkaloids from the bark of Guatteria hispida and their evaluation as antioxidant and antimicrobial agents. |
| AID574059 | Antifungal activity against 10'3 cells/ml Candida albicans ATCC 90028 by NCCLS method | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | Cell density and cell aging as factors modulating antifungal resistance of Candida albicans biofilms. |
| AID456685 | Antifungal activity against Cryptococcus neoformans ATCC 32264 assessed as inhibition of fungal growth at 12.5 uM after 48 hrs by microbroth dilution method | 2010 | Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1 | New small-size peptides possessing antifungal activity. |
| AID42855 | Inhibition of Candida albicans ATCC 44859 growth for 24 hours in vitro. | 2001 | Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17 | 3-Phenyl-5-acyloxymethyl-2H,5H-furan-2-ones: synthesis and biological activity of a novel group of potential antifungal drugs. |
| AID405055 | Antifungal activity against Sporothrix schenckii PJRC002 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by Sensititre YeastOne method | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods. |
| AID1437343 | Inhibition of CYP3A4 using in human liver microsomes using midazolam as substrate after 5 to 15 mins | |||
| AID406956 | Therapeutic index, ratio of CC50 for human K562 cells to MIC90 for Candida albicans ATCC 10261 | 2008 | Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13 | 1-[(3-Aryloxy-3-aryl)propyl]-1H-imidazoles, new imidazoles with potent activity against Candida albicans and dermatophytes. Synthesis, structure-activity relationship, and molecular modeling studies. |
| AID323059 | Antifungal activity against Saccharomyces cerevisiae ATCC 9763 by microbroth dilution method | 2008 | Bioorganic & medicinal chemistry, Jan-15, Volume: 16, Issue:2 | Antifungal and cytotoxic activities of some N-substituted aniline derivatives bearing a hetaryl fragment. |
| AID391496 | Antifungal activity against Cryptococcus neoformans ATCC 32264 after 48 hrs by spectrophotometry | 2008 | Journal of natural products, Oct, Volume: 71, Issue:10 | Evidence for the mechanism of action of the antifungal phytolaccoside B isolated from Phytolacca tetramera Hauman. |
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| AID456069 | Antifungal activity against Aspergillus versicolor ATCC 11730 after 72 hrs by serial sub-cultivation method | 2010 | Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1 | Novel 4-thiazolidinone derivatives as potential antifungal and antibacterial drugs. |
| AID404139 | Antifungal activity against Saccharomyces cerevisiae ATCC 26.01 | 2005 | Journal of natural products, Nov, Volume: 68, Issue:11 | Extraction, hemisynthesis, and synthesis of canthin-6-one analogues. Evaluation of their antifungal activities. |
| AID359387 | Antifungal activity against Candida albicans 44506 in RPMI-1640 medium after 18 to 24 hrs by twofold broth dilution method | 1992 | Journal of natural products, Nov, Volume: 55, Issue:11 | Antifungal activity of meridine, a natural product from the marine sponge Corticium sp. |
| AID553067 | Selectivity index, ratio of IC50 for human CYP11B2 to IC50 for human CYP11B1 | 2011 | ACS medicinal chemistry letters, Jan-13, Volume: 2, Issue:1 | First Selective CYP11B1 Inhibitors for the Treatment of Cortisol-Dependent Diseases. |
| AID284097 | Antifungal activity against Candida kefyr C123-2000 after 48 hrs | 2007 | Bioorganic & medicinal chemistry, Jan-01, Volume: 15, Issue:1 | Synthesis and antifungal activity of (Z)-5-arylidenerhodanines. |
| AID37718 | Minimum inhibitory concentration against Aspergillus niger | 2004 | Bioorganic & medicinal chemistry letters, Feb-09, Volume: 14, Issue:3 | Synthesis and antifungal activities of phenylenedithioureas. |
| AID50293 | In vitro minimum inhibitory concentration of compound was determined against Candida krusei after 24 hr r | 2000 | Bioorganic & medicinal chemistry letters, Aug-21, Volume: 10, Issue:16 | 3-Phenyl-5-methyl-2H,5H-furan-2-ones: tuning antifungal activity by varying substituents on the phenyl ring. |
| AID313554 | Inhibition of hepatic CYP2C19 at 10 uM | 2008 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 18, Issue:1 | Synthesis, biological evaluation and molecular modelling studies of novel ACD- and ABD-ring steroidomimetics as inhibitors of CYP17. |
| AID287716 | Cytotoxicity against human THP1 cells assessed as reduction of cell viability after 48 hrs | 2007 | Bioorganic & medicinal chemistry, Apr-01, Volume: 15, Issue:7 | Second generation of 5-ethenylbenzofuroxan derivatives as inhibitors of Trypanosoma cruzi growth: synthesis, biological evaluation, and structure-activity relationships. |
| AID566953 | Antifungal activity against Cryptococcus neoformans ATCC 32264 assessed as inhibition of fungal growth at 200 uM after 48 hrs by microplate analysis | 2011 | European journal of medicinal chemistry, Jan, Volume: 46, Issue:1 | Penetratin analogues acting as antifungal agents. |
| AID1067049 | Antifungal activity against Candida albicans Y0109 after 24 hrs by micro-broth dilution method | 2014 | European journal of medicinal chemistry, Mar-03, Volume: 74 | Synthesis, antifungal activities and molecular docking studies of novel 2-(2,4-difluorophenyl)-2-hydroxy-3-(1H-1,2,4-triazol-1-yl)propyl dithiocarbamates. |
| AID419364 | Antifungal activity against Curvularia lunata after 48 hrs by microdilution susceptibility method | 2009 | European journal of medicinal chemistry, May, Volume: 44, Issue:5 | Synthesis and bioassay of a new class of heterocycles pyrrolyl oxadiazoles/thiadiazoles/triazoles. |
| AID48236 | The compound was tested for antifungal activity against Candida pseudotropicalis MY1040 using agar dilution assay | 1987 | Journal of medicinal chemistry, Aug, Volume: 30, Issue:8 | Lysosomotropic agents. 7. Broad-spectrum antifungal activity of lysosomotropic detergents. |
| AID452370 | Inhibition of Yarrowia lipolytica 24-SMT assessed as dehydroergosterol-3-trimethylsilyl derivative at 0.2 ug/mL after 48 hrs by GC-MS analysis relative to untreated control | 2009 | Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23 | Side chain azasteroids and thiasteroids as sterol methyltransferase inhibitors in ergosterol biosynthesis. |
| AID1079941 | Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source] | |||
| AID204349 | In vitro antifungal activity against human pathogenic fungi, Sporothrix schenck ii | 2000 | Bioorganic & medicinal chemistry letters, Apr-17, Volume: 10, Issue:8 | Suitably functionalised pyrimidines as potential antimycotic agents. |
| AID255018 | Inhibitory concentration against human placental cytochrome P450 19A1 using [1-beta-3H]-androstenedione as substrate; not determined | 2005 | Journal of medicinal chemistry, Oct-20, Volume: 48, Issue:21 | Heteroaryl-substituted naphthalenes and structurally modified derivatives: selective inhibitors of CYP11B2 for the treatment of congestive heart failure and myocardial fibrosis. |
| AID340019 | Cytotoxicity against human LS174T cells assessed as viability upto 100 uM by MTT assay | 2008 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14 | Synthesis of novel ketoconazole derivatives as inhibitors of the human Pregnane X Receptor (PXR; NR1I2; also termed SXR, PAR). |
| AID625279 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID334240 | Antimicrobial activity against Cladosporium herbarum after 10 days by microdilution technique | 2002 | Journal of natural products, Apr, Volume: 65, Issue:4 | Antimicrobial activities of a new schizozygane indoline alkaloid from Schizozygia coffaeoides and the revised structure of isoschizogaline. |
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| AID600775 | Fungicidal activity against Aspergillus niger ATCC 6275 after 72 hrs | 2011 | Bioorganic & medicinal chemistry, May-15, Volume: 19, Issue:10 | Thiazole-based chalcones as potent antimicrobial agents. Synthesis and biological evaluation. |
| AID590694 | Antifungal activity against Fusarium solani after 48 hrs by microdilution method | 2011 | European journal of medicinal chemistry, Apr, Volume: 46, Issue:4 | Synthesis and biological activity of 2-(bis((1,3,4-oxadiazolyl/1,3,4-thiadiazolyl)methylthio)methylene)malononitriles. |
| AID1130374 | Antifungal activity against Microsporum canis assessed as growth inhibition in sabouraud broth after 14 days | 1979 | Journal of medicinal chemistry, Aug, Volume: 22, Issue:8 | Antimycotic imidazoles. part 4. Synthesis and antifungal activity of ketoconazole, a new potent orally active broad-spectrum antifungal agent. |
| AID380255 | Antifungal activity against Alternaria solani by MTT assay | 2006 | Journal of natural products, Dec, Volume: 69, Issue:12 | Bioactive oligostilbenoids from the stem bark of Hopea exalata. |
| AID575115 | Antifungal activity against Madurella mycetomatis isolate 54 by XTT assay | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Madurella mycetomatis is not susceptible to the echinocandin class of antifungal agents. |
| AID447227 | Antifungal activity against Candida albicans ATCC 10231 at 20 ug after 72 hrs by agar disk diffusion assay | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11 | Synthesis, Raman, FT-IR, NMR spectroscopic characterization, antimicrobial activity, cytotoxicity and DNA binding of new mixed aza-oxo-thia macrocyclic compounds. |
| AID1210013 | Inhibition of recombinant CYP2J2 (unknown origin)-mediated terfenadine hydroxylation assessed as remaining activity at 30 uM after 5 mins by LC-MS analysis relative to control | 2012 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5 | Identifying a selective substrate and inhibitor pair for the evaluation of CYP2J2 activity. |
| AID419353 | Antifungal activity against Fusarium solani at 100 ug/disk after 48 hrs by agar disc-diffusion method | 2009 | European journal of medicinal chemistry, May, Volume: 44, Issue:5 | Synthesis and bioassay of a new class of heterocycles pyrrolyl oxadiazoles/thiadiazoles/triazoles. |
| AID632562 | Antibacterial activity against Proteus vulgaris at 200 ug/mL after 24 hrs by agar cup diffusion method | 2011 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 21, Issue:24 | A new antifungal briarane diterpenoid from the gorgonian Junceella juncea Pallas. |
| AID699539 | Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake at 20 uM by scintillation counting | 2012 | Journal of medicinal chemistry, May-24, Volume: 55, Issue:10 | Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions. |
| AID284095 | Antifungal activity against Candida coliculosa C122-2000 after 48 hrs | 2007 | Bioorganic & medicinal chemistry, Jan-01, Volume: 15, Issue:1 | Synthesis and antifungal activity of (Z)-5-arylidenerhodanines. |
| AID664306 | Antifungal activity against Aspergillus clavatus MTCC 1323 by agar streak dilution method | 2012 | European journal of medicinal chemistry, Jul, Volume: 53 | Synthesis of benzimidazolyl-1,3,4-oxadiazol-2ylthio-N-phenyl (benzothiazolyl) acetamides as antibacterial, antifungal and antituberculosis agents. |
| AID406861 | Antimicrobial activity against Candida albicans SC5314 intact biofilms after 48 hrs by XTT assay | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | Role for cell density in antifungal drug resistance in Candida albicans biofilms. |
| AID532388 | Antifungal activity against Saccharomyces cerevisiae BY4741 harboring human CYP51 assessed as growth rate at 4 ug/ml (Rvb = 0.157%) | 2008 | Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10 | Differential azole antifungal efficacies contrasted using a Saccharomyces cerevisiae strain humanized for sterol 14 alpha-demethylase at the homologous locus. |
| AID1104302 | Antifungal activity against Aspergillus flavus ATCC 9643 at 28 degC measured after 72 hr by microdilution method | 2010 | Chemical & pharmaceutical bulletin, Feb, Volume: 58, Issue:2 | Sulfonamide-1,2,4-thiadiazole derivatives as antifungal and antibacterial agents: synthesis, biological evaluation, lipophilicity, and conformational studies. |
| AID363969 | Antimicrobial activity against Cryptococcus neoformans IM 961951 isolate at 6.25 ug/ml after 48 hrs | 2008 | Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17 | In vitro antifungal activity of polyfunctionalized 2-(hetero)arylquinolines prepared through imino Diels-Alder reactions. |
| AID420064 | Inhibition of human CYP3A4 assessed as biotransformation of 7-benzyloxyquinoline | 2009 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 19, Issue:12 | Selective cytochrome P450 3A4 inhibitory activity of Amaryllidaceae alkaloids. |
| AID447228 | Antifungal activity against Hanseniaspora guilliermondii DSM 3432 at 20 ug after 72 hrs by agar disk diffusion assay | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11 | Synthesis, Raman, FT-IR, NMR spectroscopic characterization, antimicrobial activity, cytotoxicity and DNA binding of new mixed aza-oxo-thia macrocyclic compounds. |
| AID771361 | Growth inhibition of human SKLU1 cells at 50 uM after 48 hrs by SRB assay relative to control | 2013 | European journal of medicinal chemistry, Oct, Volume: 68 | Cytotoxic effect of novel dehydroepiandrosterone derivatives on different cancer cell lines. |
| AID531185 | Antifungal activity against Trichophyton mentagrophytes ATCC 9533 at 9.4 uM after 5 days by CLSI method | 2008 | Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7 | Potent in vitro antifungal activities of naturally occurring acetylenic acids. |
| AID511048 | Antimicrobial activity against Fusarium solani NCIM 1330 after 48 hrs by microdilution susceptibility method | 2010 | European journal of medicinal chemistry, Sep, Volume: 45, Issue:9 | Synthesis and bioassay of aminosulfonyl-1,3,4-oxadiazoles and their interconversion to 1,3,4-thiadiazoles. |
| AID45498 | In vitro minimum inhibitory concentration of compound was determined against Candida albicans after 24 hr r | 2000 | Bioorganic & medicinal chemistry letters, Aug-21, Volume: 10, Issue:16 | 3-Phenyl-5-methyl-2H,5H-furan-2-ones: tuning antifungal activity by varying substituents on the phenyl ring. |
| AID89274 | Inhibition of Human P450 17 and NADPH-P450 reductase co-expressed in Escherichia coli with 25 uM progesterone | 2000 | Journal of medicinal chemistry, Nov-02, Volume: 43, Issue:22 | Synthesis and evaluation of novel steroidal oxime inhibitors of P450 17 (17 alpha-hydroxylase/C17-20-lyase) and 5 alpha-reductase types 1 and 2. |
| AID340963 | Antifungal activity against Cryptococcus neoformans ATCC 90112 by NCCLS M27-A2 method | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8 | Cross-resistance to medical and agricultural azole drugs in yeasts from the oropharynx of human immunodeficiency virus patients and from environmental Bavarian vine grapes. |
| AID381182 | Antifungal activity against Candida albicans after 24 to 72 hrs by disk diffusion method | 1999 | Journal of natural products, Sep, Volume: 62, Issue:9 | Antimicrobial and antitumor activities of mycosporulone. |
| AID138454 | In vivo inhibitory activity against A-23187 ear edema at a dose of 100 ug/ear | 1992 | Journal of medicinal chemistry, Aug-21, Volume: 35, Issue:17 | Novel 1-(pyridylphenyl)-1-phenyl-2-imidazolylethanols with topical antiinflammatory activity. |
| AID48463 | In vitro antifungal activity against Candida stellatoidea ATCC 36232 | 1988 | Journal of medicinal chemistry, Oct, Volume: 31, Issue:10 | Studies on antifungal agents. 23. Novel substituted 3,5-diphenyl-3-(1H-imidazol-1-ylmethyl)- 2-alkylisoxazolidine derivatives. |
| AID381185 | Antifungal activity against Candida tropicalis after 24 to 72 hrs by disk diffusion method | 1999 | Journal of natural products, Sep, Volume: 62, Issue:9 | Antimicrobial and antitumor activities of mycosporulone. |
| AID554710 | Antimicrobial activity against Candida krusei NZCDC 90.147 after 48 hrs by liquid microdilution assay | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2 | Abc1p is a multidrug efflux transporter that tips the balance in favor of innate azole resistance in Candida krusei. |
| AID102943 | Apparent receptor density at 3.16*10e-5 M concentration | 1989 | Journal of medicinal chemistry, Sep, Volume: 32, Issue:9 | LH-RH antagonists: design and synthesis of a novel series of peptidomimetics. |
| AID590624 | Antifungal activity against Aspergillus niger assessed as zone of inhibition at 100 ug/ml after 48 hrs by disc diffusion method | 2011 | European journal of medicinal chemistry, Apr, Volume: 46, Issue:4 | Synthesis and biological activity of 2-(bis((1,3,4-oxadiazolyl/1,3,4-thiadiazolyl)methylthio)methylene)malononitriles. |
| AID420076 | Antifungal activity against Cryptococcus neoformans 6995 after 24 hrs by broth microdilution assay | 2009 | Bioorganic & medicinal chemistry, Jun-01, Volume: 17, Issue:11 | Bulky 1,4-benzoxazine derivatives with antifungal activity. |
| AID1301007 | Inhibition of human recombinant CYP2C19 using CEC as substrate incubated for 50 mins by fluorimetry | 2016 | European journal of medicinal chemistry, Jul-19, Volume: 117 | 2-hydroxyisoquinoline-1,3(2H,4H)-diones (HIDs) as human immunodeficiency virus type 1 integrase inhibitors: Influence of the alkylcarboxamide substitution of position 4. |
| AID519284 | Antifungal activity against Candida parapsilosis ATCC 22019 by AFST-EUCAST method | 2008 | Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3 | Reliability of the WIDERYST susceptibility testing system for detection of in vitro antifungal resistance in yeasts. |
| AID481672 | Cytotoxicity against african green monkey Vero cells up to 25 ug/ml after 48 hrs by neutral red assay | 2010 | European journal of medicinal chemistry, May, Volume: 45, Issue:5 | Synthesis and the selective antifungal activity of 5,6,7,8-tetrahydroimidazo[1,2-a]pyridine derivatives. |
| AID511039 | Antimicrobial activity against Fusarium solani NCIM 1330 at 200 ug/disk after 48 hrs by agar disc-diffusion method | 2010 | European journal of medicinal chemistry, Sep, Volume: 45, Issue:9 | Synthesis and bioassay of aminosulfonyl-1,3,4-oxadiazoles and their interconversion to 1,3,4-thiadiazoles. |
| AID560238 | Antifungal activity against Candida albicans by checkerboard method in presence of ketoconazole | 2009 | Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8 | Curcumin modulates efflux mediated by yeast ABC multidrug transporters and is synergistic with antifungals. |
| AID1067046 | Antifungal activity against Candida parapsilosis by micro-broth dilution method | 2014 | European journal of medicinal chemistry, Mar-03, Volume: 74 | Synthesis, antifungal activities and molecular docking studies of novel 2-(2,4-difluorophenyl)-2-hydroxy-3-(1H-1,2,4-triazol-1-yl)propyl dithiocarbamates. |
| AID391494 | Antifungal activity against Candida albicans ATCC 10231 after 48 hrs by spectrophotometry | 2008 | Journal of natural products, Oct, Volume: 71, Issue:10 | Evidence for the mechanism of action of the antifungal phytolaccoside B isolated from Phytolacca tetramera Hauman. |
| AID678712 | Inhibition of human CYP1A2 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using ethoxyresorufin as substrate after 30 mins | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
| AID406955 | Therapeutic index, ratio of CC50 for human U937 cells to MIC90 for Candida albicans ATCC 10261 | 2008 | Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13 | 1-[(3-Aryloxy-3-aryl)propyl]-1H-imidazoles, new imidazoles with potent activity against Candida albicans and dermatophytes. Synthesis, structure-activity relationship, and molecular modeling studies. |
| AID1328092 | Antifungal activity against Aspergillus niger assessed as inhibition of spore germination after 48 hrs by broth dilution method | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | Synthesis and antimicrobial activity of styryl/pyrrolyl/pyrazolyl sulfonylmethyl-1,3,4-oxadiazolyl amines and styryl/pyrrolyl/pyrazolyl sulfonylmethyl-1,3,4-thiadiazolyl amines. |
| AID1467462 | Antifungal activity against Aspergillus niger at 25 ug/ml after 48 hrs by agar well diffusion method | 2017 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 27, Issue:14 | Synthesis, SAR and molecular docking studies of benzo[d]thiazole-hydrazones as potential antibacterial and antifungal agents. |
| AID531193 | Antifungal activity against Trichophyton rubrum ATCC 10218 at 9.4 uM after 5 days by CLSI method | 2008 | Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7 | Potent in vitro antifungal activities of naturally occurring acetylenic acids. |
| AID407016 | Antimicrobial activity against Cdr1, Cdr2 and Mdr1 deficient Candida albicans DSY1050 dissociated biofilms at cell density of 10'8 cells/ml after 48 hrs by XTT assay | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | Role for cell density in antifungal drug resistance in Candida albicans biofilms. |
| AID363714 | Antifungal activity against Aspergillus flavus ATCC 9170 after 48 hrs by broth microdilution technique | 2008 | Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17 | In vitro antifungal activity of polyfunctionalized 2-(hetero)arylquinolines prepared through imino Diels-Alder reactions. |
| AID214439 | In vitro minimum inhibitory concentration of compound was determined against Trichosporon beigelii after 48 hr | 2000 | Bioorganic & medicinal chemistry letters, Aug-21, Volume: 10, Issue:16 | 3-Phenyl-5-methyl-2H,5H-furan-2-ones: tuning antifungal activity by varying substituents on the phenyl ring. |
| AID1130391 | Antifungal activity against Aspergillus fumigatus assessed as growth inhibition in sabouraud broth after 14 days in presence of 10% inactivated bovine serum | 1979 | Journal of medicinal chemistry, Aug, Volume: 22, Issue:8 | Antimycotic imidazoles. part 4. Synthesis and antifungal activity of ketoconazole, a new potent orally active broad-spectrum antifungal agent. |
| AID493998 | Antifungal activity against Candida albicans ATCC 10231 assessed as inhibition of fungal growth at 100 uM | 2010 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 20, Issue:16 | New antifungal peptides. Synthesis, bioassays and initial structure prediction by CD spectroscopy. |
| AID396967 | Antifungal activity against Fusarium solani NCIM 1330 after 48 hrs by microdilution susceptibility method | 2009 | European journal of medicinal chemistry, May, Volume: 44, Issue:5 | Synthesis, antimicrobial and cytotoxic activities of 1,3,4-oxadiazoles, 1,3,4-thiadiazoles and 1,2,4-triazoles. |
| AID1275142 | Antifungal activity against clinical isolate Candida glabrata after 48 hrs by broth microdilution method | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Synthesis and biological evaluation of new naphthalene substituted thiosemicarbazone derivatives as potent antifungal and anticancer agents. |
| AID214430 | Minimum inhibitory concentration of compound for antifungal activity against Trichophyton rubrum | 2000 | Bioorganic & medicinal chemistry letters, Oct-02, Volume: 10, Issue:19 | Novel antifungals based on 4-substituted imidazole: a combinatorial chemistry approach to lead discovery and optimization. |
| AID362911 | Antifungal activity against Aspergillus niger after 24 hrs by broth microdilution method | 2008 | Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17 | NO-donors. Part 17: Synthesis and antimicrobial activity of novel ketoconazole-NO-donor hybrid compounds. |
| AID48937 | Tested for minimum inhibitory concentration against Candida albicans 124 (Candida albicans) at pH 6.5. | 1994 | Journal of medicinal chemistry, Jun-24, Volume: 37, Issue:13 | Derivatives of a novel cyclopeptolide. 1. Synthesis, antifungal activity, and structure-activity relationships. |
| AID49121 | Inhibitory activity against the Candida albicans (40 clinical isolates), determined at pH-7.2 | 1995 | Journal of medicinal chemistry, Oct-13, Volume: 38, Issue:21 | Antifungal agents. 9. 3-Aryl-4-[alpha-(1H-imidazol-1-yl)arylmethyl]pyrroles: a new class of potent anti-Candida agents. |
| AID156579 | The compound was tested for antifungal activity against Penicillium italicum MF2819 using agar dilution assay | 1987 | Journal of medicinal chemistry, Aug, Volume: 30, Issue:8 | Lysosomotropic agents. 7. Broad-spectrum antifungal activity of lysosomotropic detergents. |
| AID214271 | In vitro minimum inhibitory concentration of compound was determined against Trichophyton mentagrophytes after 72 hr | 2000 | Bioorganic & medicinal chemistry letters, Aug-21, Volume: 10, Issue:16 | 3-Phenyl-5-methyl-2H,5H-furan-2-ones: tuning antifungal activity by varying substituents on the phenyl ring. |
| AID1275143 | Antifungal activity against Candida albicans ATCC-90028 after 48 hrs by broth microdilution method | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Synthesis and biological evaluation of new naphthalene substituted thiosemicarbazone derivatives as potent antifungal and anticancer agents. |
| AID681137 | TP_TRANSPORTER: increase in Calcein-AM intracellular accumulation in mdr1a-expressing LLC-PK1 cells | 2002 | The Journal of pharmacology and experimental therapeutics, Oct, Volume: 303, Issue:1 | Interaction of cytochrome P450 3A inhibitors with P-glycoprotein. |
| AID54781 | Inhibition of recombinant human Cytochrome P450 3A4 using BFC [7-benzyloxy-4-trifluoromethylcoumarin] after 30 minutes | 2003 | Journal of medicinal chemistry, Aug-28, Volume: 46, Issue:18 | Fluorine substitution can block CYP3A4 metabolism-dependent inhibition: identification of (S)-N-[1-(4-fluoro-3- morpholin-4-ylphenyl)ethyl]-3- (4-fluorophenyl)acrylamide as an orally bioavailable KCNQ2 opener devoid of CYP3A4 metabolism-dependent inhibiti |
| AID456688 | Antifungal activity against Candida albicans ATCC 10231 assessed as inhibition of fungal growth at 200 uM after 24 hrs by microbroth dilution method | 2010 | Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1 | New small-size peptides possessing antifungal activity. |
| AID1104300 | Antifungal activity against Passalora fulva TK5318 at 28 degC measured after 72 hr by microdilution method | 2010 | Chemical & pharmaceutical bulletin, Feb, Volume: 58, Issue:2 | Sulfonamide-1,2,4-thiadiazole derivatives as antifungal and antibacterial agents: synthesis, biological evaluation, lipophilicity, and conformational studies. |
| AID454775 | Antifungal activity against Saccharomyces cerevisiae ATCC 9763 after 48 hrs by broth microdilution technique | 2009 | Bioorganic & medicinal chemistry, Nov-01, Volume: 17, Issue:21 | 5-Nitrofuranes and 5-nitrothiophenes with anti-Trypanosoma cruzi activity and ability to accumulate squalene. |
| AID1176162 | Inhibition of human recombinant MDR1 in cell membrane fraction preincubated for 5 mins at 100 uM measured after 40 mins by Pgp-Glo luciferase assay | 2015 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2 | Investigating the binding interactions of the anti-Alzheimer's drug donepezil with CYP3A4 and P-glycoprotein. |
| AID362819 | Antifungal activity against Curvularia lunata after 48 hrs by microdilution susceptibility method | 2008 | European journal of medicinal chemistry, May, Volume: 43, Issue:5 | Synthesis and antimicrobial activity of novel sulfone-linked bis heterocycles. |
| AID407005 | Antimicrobial activity against Candida albicans FH1 dissociated biofilms at cell density of 10'3 cells/ml after 48 hrs by XTT assay | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | Role for cell density in antifungal drug resistance in Candida albicans biofilms. |
| AID633913 | Antifungal activity against Aspergillus fumigatus ATCC 28212 at 10 ug/mL after 72 hrs by agar cup plate method | 2012 | European journal of medicinal chemistry, Jan, Volume: 47, Issue:1 | Isoxazoles incorporated N-substituted decahydroquinolines: a precursor to the next generation antimicrobial drug. |
| AID315659 | Inhibition of recombinant CYP2C9 at 1 uM | 2008 | Bioorganic & medicinal chemistry, Feb-15, Volume: 16, Issue:4 | Synthesis, biological evaluation and molecular modelling studies of methyleneimidazole substituted biaryls as inhibitors of human 17alpha-hydroxylase-17,20-lyase (CYP17). Part I: Heterocyclic modifications of the core structure. |
| AID330533 | Antifungal activity against Candida parapsilosis infected cyclophosphamide-immunocompromized Crl:CD1(ICR) mouse assessed as fungal density in brain at 0.5 mg/kg, po for 5 days measured on day 12 | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Mar-13, Volume: 104, Issue:11 | High-throughput synergy screening identifies microbial metabolites as combination agents for the treatment of fungal infections. |
| AID48266 | Tested In vitro for antifungal activity against candida Spp (Candida glabrata, Candida krusei) at pH 7.2 | 2002 | Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13 | Antifungal agents. 10. New derivatives of 1-[(aryl)[4-aryl-1H-pyrrol-3-yl]methyl]-1H-imidazole, synthesis, anti-candida activity, and quantitative structure-analysis relationship studies. |
| AID406960 | Antifungal activity against dermatophytes at 35 degC after 48 to 96 hrs by broth microdilution test | 2008 | Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13 | 1-[(3-Aryloxy-3-aryl)propyl]-1H-imidazoles, new imidazoles with potent activity against Candida albicans and dermatophytes. Synthesis, structure-activity relationship, and molecular modeling studies. |
| AID689076 | Antibacterial activity against Escherichia coli assessed as zone of inhibition at 0.05 mg by agar diffusion method | 2012 | Journal of natural products, Sep-28, Volume: 75, Issue:9 | Sinularosides A and B, bioactive 9,11-secosteroidal glycosides from the South China Sea soft coral Sinularia humilis Ofwegen. |
| AID1301009 | Inhibition of human recombinant CYP3A4 using BFC as substrate incubated for 30 mins by fluorimetry | 2016 | European journal of medicinal chemistry, Jul-19, Volume: 117 | 2-hydroxyisoquinoline-1,3(2H,4H)-diones (HIDs) as human immunodeficiency virus type 1 integrase inhibitors: Influence of the alkylcarboxamide substitution of position 4. |
| AID554708 | Antimicrobial activity against Candida krusei NZCDC 89.102 after 48 hrs by liquid microdilution assay | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2 | Abc1p is a multidrug efflux transporter that tips the balance in favor of innate azole resistance in Candida krusei. |
| AID1079940 | Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source] | |||
| AID405058 | Antifungal activity against Sporothrix schenckii P14036 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by Sensititre YeastOne method | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods. |
| AID1104307 | Antifungal activity against Talaromyces funiculosus ATCC 36839 at 28 degC measured after 72 hr by microdilution method | 2010 | Chemical & pharmaceutical bulletin, Feb, Volume: 58, Issue:2 | Sulfonamide-1,2,4-thiadiazole derivatives as antifungal and antibacterial agents: synthesis, biological evaluation, lipophilicity, and conformational studies. |
| AID402189 | Antifungal activity against Epidermophyton floccosum C114 after 15 days by agar dilution method | 1997 | Journal of natural products, Jul, Volume: 60, Issue:7 | In vitro evaluation of antifungal properties of 8.O.4'-neolignans. |
| AID278213 | Increased sensitivity to growth inhibition in Saccharomyces cerevisiae KLN1 carrying erg1 pL37P allele after 24 hrs relative to wild type at 30 degC | 2007 | Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1 | Characterization of squalene epoxidase of Saccharomyces cerevisiae by applying terbinafine-sensitive variants. |
| AID586923 | Resistant index, ratio of EC50 for tafenoquine-resistant promastigotes of Leishmania major R4 to EC50 for promastigotes of Leishmania major MHOM/JL/80/Friedlin | 2011 | Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3 | Increased glycolytic ATP synthesis is associated with tafenoquine resistance in Leishmania major. |
| AID402397 | Antifungal activity against Saccharomyces cerevisiae Sc7 | 1998 | Journal of natural products, Oct, Volume: 61, Issue:10 | DNA-damaging steroidal alkaloids from Eclipta alba from the suriname rainforest1. |
| AID592137 | Inhibition of human CYP17 expressed in Escherichia coli using progesterone substrate | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7 | Fine-tuning the selectivity of aldosterone synthase inhibitors: structure-activity and structure-selectivity insights from studies of heteroaryl substituted 1,2,5,6-tetrahydropyrrolo[3,2,1-ij]quinolin-4-one derivatives. |
| AID432799 | Antifungal activity against Sporothrix brasiliensis after 72 hrs by microdilution method | 2008 | Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2 | In vitro antifungal susceptibilities of five species of sporothrix. |
| AID1130385 | Antifungal activity against Staphylococcus haemolyticus assessed as growth inhibition in sabouraud broth after 14 days | 1979 | Journal of medicinal chemistry, Aug, Volume: 22, Issue:8 | Antimycotic imidazoles. part 4. Synthesis and antifungal activity of ketoconazole, a new potent orally active broad-spectrum antifungal agent. |
| AID532540 | Antifungal activity against wild-type Saccharomyces cerevisiae BY4741 assessed as accumulation of 14-alpha-methylergosta-8,24(28)-dien-3beta-6alpha-diol at 4 ug/ml | 2008 | Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10 | Differential azole antifungal efficacies contrasted using a Saccharomyces cerevisiae strain humanized for sterol 14 alpha-demethylase at the homologous locus. |
| AID244010 | Inhibition of [1-beta-2beta-3H]- -testosterone binding to human steroid 5-alpha-reductase type 2 of BPH tissue at 10 uM; - = not determined | 2005 | Journal of medicinal chemistry, Apr-21, Volume: 48, Issue:8 | Novel C-17-heteroaryl steroidal CYP17 inhibitors/antiandrogens: synthesis, in vitro biological activity, pharmacokinetics, and antitumor activity in the LAPC4 human prostate cancer xenograft model. |
| AID1176159 | Inhibition of human recombinant MDR1 in cell membrane fraction preincubated for 5 mins at 0.1 uM measured after 40 mins by Pgp-Glo luciferase assay | 2015 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2 | Investigating the binding interactions of the anti-Alzheimer's drug donepezil with CYP3A4 and P-glycoprotein. |
| AID45329 | Evaluation of In vitro antifungal activity against Candida albicans C52 by broth macro dilution method | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20 | Synthesis and antifungal activity of new azole derivatives containing an N-acylmorpholine ring. |
| AID490136 | Antifungal activity against Aspergillus niger ATCC 16404 after 24 hrs by MTT assay | 2010 | European journal of medicinal chemistry, Jul, Volume: 45, Issue:7 | Synthesis of some N-alkyl substituted urea derivatives as antibacterial and antifungal agents. |
| AID53224 | Evaluated for the inhibitory activity towards Cytochrome P450 17 rat enzyme using testicular microsome at 25 uM of substrate (progesterone) | 2000 | Journal of medicinal chemistry, Nov-02, Volume: 43, Issue:22 | Synthesis and evaluation of novel steroidal oxime inhibitors of P450 17 (17 alpha-hydroxylase/C17-20-lyase) and 5 alpha-reductase types 1 and 2. |
| AID315652 | Inhibition of human CYP17 expressed in Escherichia coli co-expressed with NADPH-P450 reductase at 1 uM | 2008 | Bioorganic & medicinal chemistry, Feb-15, Volume: 16, Issue:4 | Synthesis, biological evaluation and molecular modelling studies of methyleneimidazole substituted biaryls as inhibitors of human 17alpha-hydroxylase-17,20-lyase (CYP17). Part I: Heterocyclic modifications of the core structure. |
| AID70078 | In vitro antifungal activity against Epidermophyton floccosum ATCC E-18397 | 1988 | Journal of medicinal chemistry, Oct, Volume: 31, Issue:10 | Studies on antifungal agents. 23. Novel substituted 3,5-diphenyl-3-(1H-imidazol-1-ylmethyl)- 2-alkylisoxazolidine derivatives. |
| AID315661 | Inhibition of recombinant CYP2C19 at 1 uM | 2008 | Bioorganic & medicinal chemistry, Feb-15, Volume: 16, Issue:4 | Synthesis, biological evaluation and molecular modelling studies of methyleneimidazole substituted biaryls as inhibitors of human 17alpha-hydroxylase-17,20-lyase (CYP17). Part I: Heterocyclic modifications of the core structure. |
| AID1176936 | Antimicrobial activity against Candida tropicalis CGMCC2.3967 after 48 hrs by modified microdilution method | 2015 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3 | Synthesis, in vitro antimicrobial and cytotoxic activities of new carbazole derivatives of ursolic acid. |
| AID363744 | Antimicrobial activity against Candida albicans C129 isolate at 6.25 ug/ml after 24 hrs | 2008 | Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17 | In vitro antifungal activity of polyfunctionalized 2-(hetero)arylquinolines prepared through imino Diels-Alder reactions. |
| AID723711 | Antifungal activity against Penicillium funiculosum ATCC 36839 after 72 hrs by serial dilution technique | 2013 | Bioorganic & medicinal chemistry, Jan-15, Volume: 21, Issue:2 | Synthesis and biological evaluation of some 5-arylidene-2-(1,3-thiazol-2-ylimino)-1,3-thiazolidin-4-ones as dual anti-inflammatory/antimicrobial agents. |
| AID681358 | TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 5 uM) in Caco-2 cells | 2000 | Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 28, Issue:6 | Pharmacological inhibition of P-glycoprotein transport enhances the distribution of HIV-1 protease inhibitors into brain and testes. |
| AID1275148 | Antifungal activity against Aspergillus flavus NRRL-980 after 72 hrs by broth microdilution method | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Synthesis and biological evaluation of new naphthalene substituted thiosemicarbazone derivatives as potent antifungal and anticancer agents. |
| AID48814 | Tested for minimum inhibitory concentration against Candida tropicalis 43 (C.t) at pH 6.5. | 1994 | Journal of medicinal chemistry, Jun-24, Volume: 37, Issue:13 | Derivatives of a novel cyclopeptolide. 1. Synthesis, antifungal activity, and structure-activity relationships. |
| AID689074 | Antifungal activity against Microbotryum violaceum assessed as zone of inhibition at 0.05 mg by agar diffusion method | 2012 | Journal of natural products, Sep-28, Volume: 75, Issue:9 | Sinularosides A and B, bioactive 9,11-secosteroidal glycosides from the South China Sea soft coral Sinularia humilis Ofwegen. |
| AID572706 | Selectivity ratio, ratio of Kd for Mycobacterium smegmatis ATCC 700084 CYP164A2 to Kd for Mycobacterium tuberculosis CYP130 | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | Identification, characterization, and azole-binding properties of Mycobacterium smegmatis CYP164A2, a homolog of ML2088, the sole cytochrome P450 gene of Mycobacterium leprae. |
| AID574270 | Antifungal activity against 48 hrs cultures of 10'7 cells/ml biofilm-derived Candida albicans BF-1 planktonic cells hrs by XTT reduction method | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | Cell density and cell aging as factors modulating antifungal resistance of Candida albicans biofilms. |
| AID664304 | Antifungal activity against Aspergillus niger MTCC 282 by agar streak dilution method | 2012 | European journal of medicinal chemistry, Jul, Volume: 53 | Synthesis of benzimidazolyl-1,3,4-oxadiazol-2ylthio-N-phenyl (benzothiazolyl) acetamides as antibacterial, antifungal and antituberculosis agents. |
| AID696537 | Antifungal activity against Candida albicans ATCC 10231 after 48 hrs by broth microdilution technique | 2012 | Bioorganic & medicinal chemistry, Nov-01, Volume: 20, Issue:21 | Synthesis and antifungal activity of diverse C-2 pyridinyl and pyridinylvinyl substituted quinolines. |
| AID49460 | Antifungal activity in rat vaginal candidasis, 2 day postinfection with Candida. albicans SOB FM-391 | 1988 | Journal of medicinal chemistry, Oct, Volume: 31, Issue:10 | Studies on antifungal agents. 23. Novel substituted 3,5-diphenyl-3-(1H-imidazol-1-ylmethyl)- 2-alkylisoxazolidine derivatives. |
| AID214266 | In vitro antifungal activity against human pathogenic fungi, Trichophyton mentagrophytes | 2000 | Bioorganic & medicinal chemistry letters, Apr-17, Volume: 10, Issue:8 | Suitably functionalised pyrimidines as potential antimycotic agents. |
| AID48250 | Inhibitory activity against Candida. species. (40 clinical isolates), determined at pH-7.2 | 1995 | Journal of medicinal chemistry, Oct-13, Volume: 38, Issue:21 | Antifungal agents. 9. 3-Aryl-4-[alpha-(1H-imidazol-1-yl)arylmethyl]pyrroles: a new class of potent anti-Candida agents. |
| AID1204660 | Antifungal activity against Aspergillus fumigatus assessed as growth inhibition at 0.5 mg/ml after 48 hrs by well diffusion method | 2015 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 25, Issue:12 | Isolation, semi-synthesis and bio-evaluation of spatane derivatives from the brown algae Stoechospermum marginatum. |
| AID158620 | Inhibitory activity against phospholipase A2 of Croatalus adamanteus | 1992 | Journal of medicinal chemistry, Aug-21, Volume: 35, Issue:17 | Novel 1-(pyridylphenyl)-1-phenyl-2-imidazolylethanols with topical antiinflammatory activity. |
| AID554728 | Inhibition of Candida krusei ABC1 expressed in Saccharomyces cerevisiae isolate ADdelta at 0.28 nM | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2 | Abc1p is a multidrug efflux transporter that tips the balance in favor of innate azole resistance in Candida krusei. |
| AID1079934 | Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source] | |||
| AID588217 | FDA HLAED, serum glutamic pyruvic transaminase (SGPT) increase | 2004 | Current drug discovery technologies, Dec, Volume: 1, Issue:4 | Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling. |
| AID50296 | Minimum inhibitory concentration of compound for antifungal activity against Candida krusei | 2000 | Bioorganic & medicinal chemistry letters, Oct-02, Volume: 10, Issue:19 | Novel antifungals based on 4-substituted imidazole: a combinatorial chemistry approach to lead discovery and optimization. |
| AID1110740 | Antifungal activity against Trichosporon beigelii 1188 after 24 hr by microdilution broth method | 2002 | Farmaco (Societa chimica italiana : 1989), Feb, Volume: 57, Issue:2 | Ring substituted 3-phenyl-1-(2-pyrazinyl)-2-propen-1-ones as potential photosynthesis-inhibiting, antifungal and antimycobacterial agents. |
| AID530964 | Antifungal activity against Fluconazole resistant Candida albicans clinical isolate 17 after 48 hrs by CLSI method | 2008 | Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7 | Potent in vitro antifungal activities of naturally occurring acetylenic acids. |
| AID330522 | Antifungal activity against Candida parapsilosis infected cyclophosphamide-immunocompromized Crl:CD1(ICR) mouse assessed as survival at 0.5 mg/kg, po for 5 days in presence of beauvericin | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Mar-13, Volume: 104, Issue:11 | High-throughput synergy screening identifies microbial metabolites as combination agents for the treatment of fungal infections. |
| AID666779 | Antibacterial activity against Bacillus megaterium at 0.05 mg by agar diffusion test | 2012 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 22, Issue:13 | Bioactive briarane diterpenoids from the South China Sea gorgonian Dichotella gemmacea. |
| AID330524 | Antifungal activity against Candida parapsilosis infected cyclophosphamide-immunocompromized Crl:CD1(ICR) mouse assessed as survival at 50 mg/kg, po for 5 days | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Mar-13, Volume: 104, Issue:11 | High-throughput synergy screening identifies microbial metabolites as combination agents for the treatment of fungal infections. |
| AID600769 | Antifungal activity against Trichoderma viride IAM 5061 after 72 hrs by serial dilution method | 2011 | Bioorganic & medicinal chemistry, May-15, Volume: 19, Issue:10 | Thiazole-based chalcones as potent antimicrobial agents. Synthesis and biological evaluation. |
| AID1328083 | Antifungal activity against Penicillium chrysogenum assessed as inhibition of spore germination at 25 ug/well after 48 hrs by agar well diffusion method | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | Synthesis and antimicrobial activity of styryl/pyrrolyl/pyrazolyl sulfonylmethyl-1,3,4-oxadiazolyl amines and styryl/pyrrolyl/pyrazolyl sulfonylmethyl-1,3,4-thiadiazolyl amines. |
| AID554706 | Antimicrobial activity against Candida krusei IFO0011 after 48 hrs by liquid microdilution assay | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2 | Abc1p is a multidrug efflux transporter that tips the balance in favor of innate azole resistance in Candida krusei. |
| AID555136 | Antimicrobial activity against Candida albicans by CLSI M27-A2 broth microdilution method | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Fenticonazole activity measured by the methods of the European Committee on Antimicrobial Susceptibility Testing and CLSI against 260 Candida vulvovaginitis isolates from two European regions and annotations on the prevalent genotypes. |
| AID429373 | Antifungal activity against Trichoderma viride after 72 hrs by liquid dilution method | 2009 | European journal of medicinal chemistry, Aug, Volume: 44, Issue:8 | Mono and bis-6-arylbenzimidazo[1,2-c]quinazolines: a new class of antimicrobial agents. |
| AID644186 | Antifungal activity against Aspergillus versicolor ATCC 11730 after 72 hrs by serial dilution method | 2012 | Bioorganic & medicinal chemistry, Feb-15, Volume: 20, Issue:4 | Synthesis of novel sulfonamide-1,2,4-triazoles, 1,3,4-thiadiazoles and 1,3,4-oxadiazoles, as potential antibacterial and antifungal agents. Biological evaluation and conformational analysis studies. |
| AID1061739 | Antimicrobial activity against Candida glabrata by broth microdilution method | 2014 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1 | Synthesis and evaluation of novel azoles as potent antifungal agents. |
| AID530947 | Antifungal activity against Trichophyton rubrum ATCC MYA-4438 by CLSI method | 2008 | Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7 | Potent in vitro antifungal activities of naturally occurring acetylenic acids. |
| AID515180 | Antimicrobial activity against Trichophyton rubrum ATCC 10218 after 48 hrs by modified microdilution method | 2010 | European journal of medicinal chemistry, Oct, Volume: 45, Issue:10 | Synthesis and antimicrobial activities of novel 1H-dibenzo[a,c]carbazoles from dehydroabietic acid. |
| AID1129511 | Antimicrobial activity against Penicillium chrysogenum at 50 ug/well after 48 hrs by agar well diffusion method | 2014 | European journal of medicinal chemistry, Apr-22, Volume: 77 | Synthesis, antimicrobial and cytotoxic activities of pyrimidinyl benzoxazole, benzothiazole and benzimidazole. |
| AID1557078 | Antifungal activity against Candida glabrata ATCC 66032 assessed as reduction in fungal cell growth incubated for 24 hrs by MTT based broth double dilution method | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Antifungal activity, mode of action variability, and subcellular distribution of coumarin-based antifungal azoles. |
| AID45502 | In vivo Evaluation of minimum inhibitory concentration against Candida albicans 406 | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20 | Synthesis and antifungal activity of new azole derivatives containing an N-acylmorpholine ring. |
| AID723704 | Fungicidal activity against Trichoderma viride IAM 5061 after 72 hrs by serial subcultivation method | 2013 | Bioorganic & medicinal chemistry, Jan-15, Volume: 21, Issue:2 | Synthesis and biological evaluation of some 5-arylidene-2-(1,3-thiazol-2-ylimino)-1,3-thiazolidin-4-ones as dual anti-inflammatory/antimicrobial agents. |
| AID396969 | Antifungal activity against Aspergillus niger NCIM 596 after 48 hrs by microdilution susceptibility method | 2009 | European journal of medicinal chemistry, May, Volume: 44, Issue:5 | Synthesis, antimicrobial and cytotoxic activities of 1,3,4-oxadiazoles, 1,3,4-thiadiazoles and 1,2,4-triazoles. |
| AID1496821 | Inhibition of CYP3A4 in human liver microsomes assessed as midazolam 1'-hydroxylation after 4 to 40 mins in presence of NADPH by LCMS analysis | 2018 | Bioorganic & medicinal chemistry, 07-15, Volume: 26, Issue:11 | Synthesis and profiling of benzylmorpholine 1,2,4,5-tetraoxane analogue N205: Towards tetraoxane scaffolds with potential for single dose cure of malaria. |
| AID415950 | Antimicrobial activity against Cryptococcus neoformans by micro-broth dilution method | 2009 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6 | Design, synthesis, and biological evaluation of novel 1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluorophenyl)-3-substituted benzylamino-2-propanols. |
| AID42869 | Inhibition of Candida glabrata 20/I growth for 48 hours in vitro. | 2001 | Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17 | 3-Phenyl-5-acyloxymethyl-2H,5H-furan-2-ones: synthesis and biological activity of a novel group of potential antifungal drugs. |
| AID417964 | Antimicrobial activity against Aspergillus flavus after 48 hrs by broth microdilution technique | 2009 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6 | Relation between lipophilicity of alkyl gallates and antifungal activity against yeasts and filamentous fungi. |
| AID537735 | Binding affinity to Candida albicans CaMdr1p expressed in yeast AD1-8u | 2010 | European journal of medicinal chemistry, Nov, Volume: 45, Issue:11 | Analysis of physico-chemical properties of substrates of ABC and MFS multidrug transporters of pathogenic Candida albicans. |
| AID633951 | Antifungal activity against Aspergillus fumigatus isolated from human after 72 hrs by serial dilution technique | 2011 | Bioorganic & medicinal chemistry, Dec-15, Volume: 19, Issue:24 | Novel (E)-1-(4-methyl-2-(alkylamino)thiazol-5-yl)-3-arylprop-2-en-1-ones as potent antimicrobial agents. |
| AID1171991 | Antibacterial activity against Enterobacter aerogenes MTCC 111 assessed as inhibition of visual growth after 24 hrs | 2015 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2 | Facile and diastereoselective synthesis of 3,2'-spiropyrrolidine-oxindoles derivatives, their molecular docking and antiproliferative activities. |
| AID563613 | Effect on sterol composition in Candida albicans isolate 108 harboring erg11 and erg5 double mutant assessed as 14 -Methylergosta-8,24(28)-dien-3beta,6alpha-diol level after 2 hrs by gas chromatography | 2010 | Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9 | A clinical isolate of Candida albicans with mutations in ERG11 (encoding sterol 14alpha-demethylase) and ERG5 (encoding C22 desaturase) is cross resistant to azoles and amphotericin B. |
| AID530950 | Antifungal activity against Trichophyton mentagrophytes ATCC 9533 by CLSI method | 2008 | Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7 | Potent in vitro antifungal activities of naturally occurring acetylenic acids. |
| AID618043 | Antifungal activity against 10'5 CFU/mL Aspergillus fumigatus MTCC 343 at 100 ug/ml after 48 hrs by disc diffusion technique | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Synthesis and studies of novel 2-(4-cyano-3-trifluoromethylphenyl amino)-4-(quinoline-4-yloxy)-6-(piperazinyl/piperidinyl)-s-triazines as potential antimicrobial, antimycobacterial and anticancer agents. |
| AID48597 | Minimum inhibitory concentration against Candida albicans | 2004 | Bioorganic & medicinal chemistry letters, Jan-19, Volume: 14, Issue:2 | Synthesis of galactopyranosyl amino alcohols as a new class of antitubercular and antifungal agents. |
| AID1321758 | Inhibition of CYP3A4 in pooled human hepatic microsomes using testosterone substrate in presence of NADPH | |||
| AID48824 | Tested for minimum subinhibitory concentration against Candida tropicalis 43 (C.t) at pH 6.5. | 1994 | Journal of medicinal chemistry, Jun-24, Volume: 37, Issue:13 | Derivatives of a novel cyclopeptolide. 1. Synthesis, antifungal activity, and structure-activity relationships. |
| AID334241 | Antimicrobial activity against Candida albicans after 24 hrs by microdilution technique | 2002 | Journal of natural products, Apr, Volume: 65, Issue:4 | Antimicrobial activities of a new schizozygane indoline alkaloid from Schizozygia coffaeoides and the revised structure of isoschizogaline. |
| AID1130380 | Antifungal activity against Aspergillus fumigatus assessed as growth inhibition in sabouraud broth after 14 days | 1979 | Journal of medicinal chemistry, Aug, Volume: 22, Issue:8 | Antimycotic imidazoles. part 4. Synthesis and antifungal activity of ketoconazole, a new potent orally active broad-spectrum antifungal agent. |
| AID285160 | Antimicrobial activity against non replicating persistence Mycobacterium tuberculosis H37Rv in aerobic condition assessed as bacterial density after 7 days | 2007 | Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4 | Low-oxygen-recovery assay for high-throughput screening of compounds against nonreplicating Mycobacterium tuberculosis. |
| AID717028 | Antifungal activity against Candida albicans ATCC 90028 after 24 hrs by microdilution susceptibility assay | 2012 | European journal of medicinal chemistry, Dec, Volume: 58 | Synthesis and biological evaluation of some hydrazone derivatives as new anticandidal and anticancer agents. |
| AID2916 | Inhibition of cytochrome P450 progesterone 15-alpha hydroxylase | 1992 | Journal of medicinal chemistry, Jul-24, Volume: 35, Issue:15 | Stereoisomers of ketoconazole: preparation and biological activity. |
| AID420211 | Antimicrobial activity against Candida albicans UFPEDA 1007 at 25 ug/disk after 48 hrs by disk diffusion method | 2009 | European journal of medicinal chemistry, May, Volume: 44, Issue:5 | Synthesis, antimicrobial and cytotoxic activities of some 5-arylidene-4-thioxo-thiazolidine-2-ones. |
| AID330534 | Antifungal activity against Candida parapsilosis infected cyclophosphamide-immunocompromized Crl:CD1(ICR) mouse assessed as fungal density in brain at 0.5 mg/kg, po for 5 days measured on day 12 in presence beauvericin | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Mar-13, Volume: 104, Issue:11 | High-throughput synergy screening identifies microbial metabolites as combination agents for the treatment of fungal infections. |
| AID417963 | Antimicrobial activity against Aspergillus fumigatus after 48 hrs by broth microdilution technique | 2009 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6 | Relation between lipophilicity of alkyl gallates and antifungal activity against yeasts and filamentous fungi. |
| AID377678 | Antifungal activity against filamentous Wangiella dermatitidis after 48 hrs by NCCLS M27A method | 2006 | Journal of natural products, Jul, Volume: 69, Issue:7 | Phytochemistry and antifungal properties of the newly discovered tree Pleodendron costaricense. |
| AID397743 | Inhibition of human ERG channel | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14 | Side chain flexibilities in the human ether-a-go-go related gene potassium channel (hERG) together with matched-pair binding studies suggest a new binding mode for channel blockers. |
| AID53243 | Inhibition of rat testicular microsomal Cytochrome P450 17A1 | 1997 | Journal of medicinal chemistry, Sep-26, Volume: 40, Issue:20 | 17-Imidazolyl, pyrazolyl, and isoxazolyl androstene derivatives. Novel steroidal inhibitors of human cytochrome C17,20-lyase (P450(17 alpha). |
| AID664305 | Antifungal activity against Aspergillus fumigatus MTCC 343 by agar streak dilution method | 2012 | European journal of medicinal chemistry, Jul, Volume: 53 | Synthesis of benzimidazolyl-1,3,4-oxadiazol-2ylthio-N-phenyl (benzothiazolyl) acetamides as antibacterial, antifungal and antituberculosis agents. |
| AID1079933 | Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is | |||
| AID1435414 | Anti-bacterial activity against Staphylococcus aureus ATCC 10832 measured after 24 hrs by microtiter broth dilution method | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Design, synthesis and antimicrobial evaluation of novel benzoxazole derivatives. |
| AID334243 | Antimicrobial activity against Staphylococcus aureus NCIMB 9515 after 24 hrs by microdilution technique | 2002 | Journal of natural products, Apr, Volume: 65, Issue:4 | Antimicrobial activities of a new schizozygane indoline alkaloid from Schizozygia coffaeoides and the revised structure of isoschizogaline. |
| AID1110733 | Antifungal activity against Lichtheimia corymbifera 272 after 48 hr by microdilution broth method | 2002 | Farmaco (Societa chimica italiana : 1989), Feb, Volume: 57, Issue:2 | Ring substituted 3-phenyl-1-(2-pyrazinyl)-2-propen-1-ones as potential photosynthesis-inhibiting, antifungal and antimycobacterial agents. |
| AID340015 | Induction of PXR transactivation in HepG2 cells | 2008 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14 | Synthesis of novel ketoconazole derivatives as inhibitors of the human Pregnane X Receptor (PXR; NR1I2; also termed SXR, PAR). |
| AID2935 | Inhibition of cytochrome P450 progesterone 16-alpha hydroxylase | 1992 | Journal of medicinal chemistry, Jul-24, Volume: 35, Issue:15 | Stereoisomers of ketoconazole: preparation and biological activity. |
| AID594165 | Antimicrobial activity against Aspergillus niger after 48 hrs by agar well diffusion method | 2011 | European journal of medicinal chemistry, May, Volume: 46, Issue:5 | Synthesis, antimicrobial, antioxidant, anti-hemolytic and cytotoxic evaluation of new imidazole-based heterocycles. |
| AID574267 | Antifungal activity against 24 hrs cultures of 10'7 cells/ml biofilm-derived Candida albicans ATCC 90028 planktonic cells hrs by XTT reduction method | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | Cell density and cell aging as factors modulating antifungal resistance of Candida albicans biofilms. |
| AID566952 | Antifungal activity against Candida albicans ATCC 10231 assessed as inhibition of fungal growth at 6.25 uM after 24 hrs by microplate analysis | 2011 | European journal of medicinal chemistry, Jan, Volume: 46, Issue:1 | Penetratin analogues acting as antifungal agents. |
| AID530955 | Antifungal activity against Aspergillus flavus ATCC 204304 after 5 days by CLSI method | 2008 | Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7 | Potent in vitro antifungal activities of naturally occurring acetylenic acids. |
| AID207274 | Inhibition of Steroid 17-alpha-hydroxylase/17,20 lyase from rat testes microsomal preparation | 1990 | Journal of medicinal chemistry, Sep, Volume: 33, Issue:9 | Hydroxyperfluoroazobenzenes: novel inhibitors of enzymes of androgen biosynthesis. |
| AID1196739 | Antifungal activity against Aspergillus flavus NRRL 980 after 72 hrs by broth microdilution assay | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | A novel series of thiazolyl-pyrazoline derivatives: synthesis and evaluation of antifungal activity, cytotoxicity and genotoxicity. |
| AID1196742 | Antifungal activity against Fusarium solani NRRL 13414 after 72 hrs by broth microdilution assay | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | A novel series of thiazolyl-pyrazoline derivatives: synthesis and evaluation of antifungal activity, cytotoxicity and genotoxicity. |
| AID395650 | Antifungal activity against Candida albicans ATCC 10231 assessed as growth inhibition at 12.5 uM after 24 hrs | 2009 | European journal of medicinal chemistry, Jan, Volume: 44, Issue:1 | Penetratin and derivatives acting as antifungal agents. |
| AID613257 | Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 700699 after 24 hrs by NCCLS M7-A6 broth dilution method | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Design, synthesis and antimicrobial activity of chiral 2-(substituted-hydroxyl)-3-(benzo[d]oxazol-5-yl)propanoic acid derivatives. |
| AID482321 | Inhibition of aromatase from human placental microsomes at 10 uM | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Novel highly potent and selective nonsteroidal aromatase inhibitors: synthesis, biological evaluation and structure-activity relationships investigation. |
| AID1130384 | Antifungal activity against Erysipelothrix insidiosa assessed as growth inhibition in sabouraud broth after 14 days | 1979 | Journal of medicinal chemistry, Aug, Volume: 22, Issue:8 | Antimycotic imidazoles. part 4. Synthesis and antifungal activity of ketoconazole, a new potent orally active broad-spectrum antifungal agent. |
| AID284096 | Antifungal activity against Candida krusei C117-2000 after 48 hrs | 2007 | Bioorganic & medicinal chemistry, Jan-01, Volume: 15, Issue:1 | Synthesis and antifungal activity of (Z)-5-arylidenerhodanines. |
| AID405094 | Antimicrobial activity against Rhizopus microsporus var. rhizopodiformis after 24 hrs | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | In vitro susceptibilities of 217 clinical isolates of zygomycetes to conventional and new antifungal agents. |
| AID54876 | Evaluation of In vitro antifungal activity against Cryptococcus neoformans 74 by broth macro dilution method | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20 | Synthesis and antifungal activity of new azole derivatives containing an N-acylmorpholine ring. |
| AID1110744 | Antifungal activity against Candida tropicalis 156 after 48 hr by microdilution broth method | 2002 | Farmaco (Societa chimica italiana : 1989), Feb, Volume: 57, Issue:2 | Ring substituted 3-phenyl-1-(2-pyrazinyl)-2-propen-1-ones as potential photosynthesis-inhibiting, antifungal and antimycobacterial agents. |
| AID600766 | Antifungal activity against Aspergillus versicolor ATCC 11730 after 72 hrs by serial dilution method | 2011 | Bioorganic & medicinal chemistry, May-15, Volume: 19, Issue:10 | Thiazole-based chalcones as potent antimicrobial agents. Synthesis and biological evaluation. |
| AID1467463 | Antifungal activity against Aspergillus niger at 50 ug/ml after 48 hrs by agar well diffusion method | 2017 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 27, Issue:14 | Synthesis, SAR and molecular docking studies of benzo[d]thiazole-hydrazones as potential antibacterial and antifungal agents. |
| AID510165 | Antifungal activity against Candida albicans ATCC 10231 by spectrophotometry | 2010 | European journal of medicinal chemistry, Sep, Volume: 45, Issue:9 | A study of cytotoxicity of novel chlorokojic acid derivatives with their antimicrobial and antiviral activities. |
| AID43431 | Compound was tested for the inhibition of beta-lactamase | 2003 | Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21 | Identification and prediction of promiscuous aggregating inhibitors among known drugs. |
| AID377675 | Antifungal activity against Cryptococcus neoformans after 48 hrs by NCCLS M27A method | 2006 | Journal of natural products, Jul, Volume: 69, Issue:7 | Phytochemistry and antifungal properties of the newly discovered tree Pleodendron costaricense. |
| AID574271 | Ratio of MIC for 10'8 cells/ml wild-type Candida albicans BF-1 to MIC for 10'7 cells/ml wild-type Candida albicans BF-1 grown as planktonic cells | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | Cell density and cell aging as factors modulating antifungal resistance of Candida albicans biofilms. |
| AID456841 | Antifungal activity against Aspergillus fumigatus clinical isolate after 72 hrs by serial sub-cultivation method | 2010 | Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1 | Novel 4-thiazolidinone derivatives as potential antifungal and antibacterial drugs. |
| AID125808 | In vitro antifungal activity against Microsporum canis | 1984 | Journal of medicinal chemistry, Jul, Volume: 27, Issue:7 | Antimycotic azoles. 7. Synthesis and antifungal properties of a series of novel triazol-3-ones. |
| AID1110749 | Antifungal activity against Trichophyton mentagrophytes 445 after 72 hr by microdilution broth method | 2002 | Farmaco (Societa chimica italiana : 1989), Feb, Volume: 57, Issue:2 | Ring substituted 3-phenyl-1-(2-pyrazinyl)-2-propen-1-ones as potential photosynthesis-inhibiting, antifungal and antimycobacterial agents. |
| AID644194 | Antifungal activity against Aspergillus versicolor ATCC 11730 treated for 72 hrs followed by sub-cultivated for 5 days by serial dilution method | 2012 | Bioorganic & medicinal chemistry, Feb-15, Volume: 20, Issue:4 | Synthesis of novel sulfonamide-1,2,4-triazoles, 1,3,4-thiadiazoles and 1,3,4-oxadiazoles, as potential antibacterial and antifungal agents. Biological evaluation and conformational analysis studies. |
| AID1196737 | Antifungal activity against Candida zeylanoides NRLL Y 1774 after 48 hrs by broth microdilution assay | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | A novel series of thiazolyl-pyrazoline derivatives: synthesis and evaluation of antifungal activity, cytotoxicity and genotoxicity. |
| AID1157297 | Antifungal activity against Microsporum gypseum Cmccfmza assessed as growth inhibition by automatic microplate reader analysis | 2014 | Journal of natural products, May-23, Volume: 77, Issue:5 | Polyhydroxy cyclohexanols from a Dendrodochium sp. fungus associated with the sea cucumber Holothuria nobilis Selenka. |
| AID49095 | The compound was tested for antifungal activity against Candida albicans MY1058 using agar dilution assay | 1987 | Journal of medicinal chemistry, Aug, Volume: 30, Issue:8 | Lysosomotropic agents. 7. Broad-spectrum antifungal activity of lysosomotropic detergents. |
| AID340966 | Antifungal activity against Rhodotorula sp. isolates from grapes by NCCLS M27-A2 method | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8 | Cross-resistance to medical and agricultural azole drugs in yeasts from the oropharynx of human immunodeficiency virus patients and from environmental Bavarian vine grapes. |
| AID405104 | Antimicrobial activity against Rhizopus arrhizus assessed as percent of susceptible isolates after 24 hrs | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | In vitro susceptibilities of 217 clinical isolates of zygomycetes to conventional and new antifungal agents. |
| AID699540 | Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake at 20 uM incubated for 5 mins by scintillation counting | 2012 | Journal of medicinal chemistry, May-24, Volume: 55, Issue:10 | Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions. |
| AID1435413 | Anti-bacterial activity against Escherichia coli ATCC 11303 measured after 24 hrs by microtiter broth dilution method | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Design, synthesis and antimicrobial evaluation of novel benzoxazole derivatives. |
| AID1275151 | Antifungal activity against Fusarium solani NRRL-13414 after 72 hrs by broth microdilution method | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Synthesis and biological evaluation of new naphthalene substituted thiosemicarbazone derivatives as potent antifungal and anticancer agents. |
| AID294850 | Antifungal activity against Candida tropicalis after 7 days by micro-broth dilution method | 2007 | European journal of medicinal chemistry, Sep, Volume: 42, Issue:9 | Synthesis of novel triazole derivatives as inhibitors of cytochrome P450 14alpha-demethylase (CYP51). |
| AID456839 | Antifungal activity against Trichoderma viride IAM 5061 after 72 hrs by serial sub-cultivation method | 2010 | Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1 | Novel 4-thiazolidinone derivatives as potential antifungal and antibacterial drugs. |
| AID1247086 | Antifungal activity against Aspergillus flavus assessed as growth inhibition at 1 mg/well after 48 hrs by Well method | 2015 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19 | Synthesis of BF₃ catalyzed Mannich derivatives with excellent ee from phenylpropanolamine, study of their antimicrobial activity and molecular docking. |
| AID530736 | Antifungal activity against Candida albicans ATCC 60193 at 9.4 uM after 48 hrs by CLSI method | 2008 | Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7 | Potent in vitro antifungal activities of naturally occurring acetylenic acids. |
| AID1319284 | Inhibition of CYP3A4 in human liver microsomes using midazolam as substrate assessed as reduction in 4-OH-midazolam formation by LC/MS/MS analysis | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18 | Identification of (R)-(2-Chloro-3-(trifluoromethyl)phenyl)(1-(5-fluoropyridin-2-yl)-4-methyl-6,7-dihydro-1H-imidazo[4,5-c]pyridin-5(4H)-yl)methanone (JNJ 54166060), a Small Molecule Antagonist of the P2X7 receptor. |
| AID618042 | Antifungal activity against 10'5 CFU/mL Aspergillus niger MTCC 282 at 100 ug/ml after 48 hrs by disc diffusion technique | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Synthesis and studies of novel 2-(4-cyano-3-trifluoromethylphenyl amino)-4-(quinoline-4-yloxy)-6-(piperazinyl/piperidinyl)-s-triazines as potential antimicrobial, antimycobacterial and anticancer agents. |
| AID415949 | Antimicrobial activity against Candida albicans by micro-broth dilution method | 2009 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6 | Design, synthesis, and biological evaluation of novel 1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluorophenyl)-3-substituted benzylamino-2-propanols. |
| AID270823 | Inhibition of rat testis 17-alpha-hydroxylase component of P450-17alpha | 2006 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 16, Issue:18 | Synthesis, biochemical evaluation and rationalisation of the inhibitory activity of a range of 4-substituted phenyl alkyl imidazole-based inhibitors of the enzyme complex 17alpha-hydroxylase/17,20-lyase (P450(17alpha)). |
| AID302123 | Antifungal activity against fluconazole-resistant Candida albicans 01010 after 24 hrs | 2007 | Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22 | Synthesis and antifungal activities of novel 2-aminotetralin derivatives. |
| AID572707 | Selectivity ratio, ratio of Kd for Mycobacterium smegmatis ATCC 700084 CYP164A2 to Kd for Mycobacterium tuberculosis CYP51 | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | Identification, characterization, and azole-binding properties of Mycobacterium smegmatis CYP164A2, a homolog of ML2088, the sole cytochrome P450 gene of Mycobacterium leprae. |
| AID42868 | Inhibition of Candida glabrata 20/I growth for 24 hours in vitro. | 2001 | Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17 | 3-Phenyl-5-acyloxymethyl-2H,5H-furan-2-ones: synthesis and biological activity of a novel group of potential antifungal drugs. |
| AID340952 | Antifungal activity against Candida albicans isolates by NCCLS M27-A2 method | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8 | Cross-resistance to medical and agricultural azole drugs in yeasts from the oropharynx of human immunodeficiency virus patients and from environmental Bavarian vine grapes. |
| AID590695 | Antifungal activity against Curvularia lunata after 48 hrs by microdilution method | 2011 | European journal of medicinal chemistry, Apr, Volume: 46, Issue:4 | Synthesis and biological activity of 2-(bis((1,3,4-oxadiazolyl/1,3,4-thiadiazolyl)methylthio)methylene)malononitriles. |
| AID696545 | Antifungal activity against Trichophyton mentagrophytes ATCC 9972 after 48 hrs by broth microdilution technique | 2012 | Bioorganic & medicinal chemistry, Nov-01, Volume: 20, Issue:21 | Synthesis and antifungal activity of diverse C-2 pyridinyl and pyridinylvinyl substituted quinolines. |
| AID574264 | Antifungal activity against 24 hrs cultures of 10'7 cells/ml Candida albicans BF-1 biofilms by XTT reduction method | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | Cell density and cell aging as factors modulating antifungal resistance of Candida albicans biofilms. |
| AID644184 | Antifungal activity against Aspergillus niger ATCC 6275 after 72 hrs by serial dilution method | 2012 | Bioorganic & medicinal chemistry, Feb-15, Volume: 20, Issue:4 | Synthesis of novel sulfonamide-1,2,4-triazoles, 1,3,4-thiadiazoles and 1,3,4-oxadiazoles, as potential antibacterial and antifungal agents. Biological evaluation and conformational analysis studies. |
| AID49112 | 50% inhibitory activity against Candida albicans (40 clinical isolates) determined at pH-7.2 | 1995 | Journal of medicinal chemistry, Oct-13, Volume: 38, Issue:21 | Antifungal agents. 9. 3-Aryl-4-[alpha-(1H-imidazol-1-yl)arylmethyl]pyrroles: a new class of potent anti-Candida agents. |
| AID330526 | Antifungal activity against Candida parapsilosis infected cyclophosphamide-immunocompromized Crl:CD1(ICR) mouse assessed as fungal density in kidney at 0.5 mg/kg, po for 5 days measured on day 12 in presence beauvericin | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Mar-13, Volume: 104, Issue:11 | High-throughput synergy screening identifies microbial metabolites as combination agents for the treatment of fungal infections. |
| AID45485 | In vitro antifungal activity against human pathogenic fungi, Candida albicans | 2000 | Bioorganic & medicinal chemistry letters, Apr-17, Volume: 10, Issue:8 | Suitably functionalised pyrimidines as potential antimycotic agents. |
| AID420072 | Antifungal activity against Candida glabrata after 24 hrs by broth microdilution assay | 2009 | Bioorganic & medicinal chemistry, Jun-01, Volume: 17, Issue:11 | Bulky 1,4-benzoxazine derivatives with antifungal activity. |
| AID596443 | Antifungal activity against Candida albicans ATCC 10213 | 2011 | Bioorganic & medicinal chemistry, May-01, Volume: 19, Issue:9 | Antifungal, cytotoxic and SAR studies of a series of N-alkyl, N-aryl and N-alkylphenyl-1,4-pyrrolediones and related compounds. |
| AID322157 | Antifungal activity against Candida albicans C 129-2000 after 48 hrs by CLSI M27-A2 method | 2008 | Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1 | N-Phenyl and N-phenylalkyl-maleimides acting against Candida spp.: time-to-kill, stability, interaction with maleamic acids. |
| AID1317746 | Inhibition of Wistar rat testicular C17,20-lyase assessed as androst-4-ene-3,17-dione formation using [3H]17-hydroxyprogesterone as substrate in presence of NADPH | 2016 | European journal of medicinal chemistry, Sep-14, Volume: 120 | Synthesis of novel 17-(4'-formyl)pyrazolylandrosta-5,16-dienes and their derivatives as potent 17α-hydroxylase/C17,20-lyase inhibitors or antiproliferative agents depending on the substitution pattern of the heteroring. |
| AID555138 | Antimicrobial activity against Candida parapsilosis ATCC 22019 by EUCAST broth microdilution method | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Fenticonazole activity measured by the methods of the European Committee on Antimicrobial Susceptibility Testing and CLSI against 260 Candida vulvovaginitis isolates from two European regions and annotations on the prevalent genotypes. |
| AID420077 | Antifungal activity against Cryptococcus neoformans 6995 after 48 hrs by broth microdilution assay | 2009 | Bioorganic & medicinal chemistry, Jun-01, Volume: 17, Issue:11 | Bulky 1,4-benzoxazine derivatives with antifungal activity. |
| AID1332948 | Antifungal activity against Aspergillus niger MTCC 1881 measured after 2 days by broth dilution method | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Synthesis, antimicrobial activity and advances in structure-activity relationships (SARs) of novel tri-substituted thiazole derivatives. |
| AID456838 | Antifungal activity against Trichoderma viride IAM 5061 after 72 hrs by serial dilution method | 2010 | Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1 | Novel 4-thiazolidinone derivatives as potential antifungal and antibacterial drugs. |
| AID49092 | The compound was tested for antifungal activity against Candida albicans MY0992 using agar dilution assay | 1987 | Journal of medicinal chemistry, Aug, Volume: 30, Issue:8 | Lysosomotropic agents. 7. Broad-spectrum antifungal activity of lysosomotropic detergents. |
| AID303384 | Selectivity index, ratio of IC50 for human THP1 cells to IC50 for Trypanosoma cruzi Y | 2007 | Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24 | In vivo anti-Chagas vinylthio-, vinylsulfinyl-, and vinylsulfonylbenzofuroxan derivatives. |
| AID456071 | Antifungal activity against Aspergillus flavus ATCC 9643 after 72 hrs by serial sub-cultivation method | 2010 | Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1 | Novel 4-thiazolidinone derivatives as potential antifungal and antibacterial drugs. |
| AID282733 | Inhibition of all-trans retinoic acid metabolism in rat liver microsomes | 2005 | Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23 | Novel tetralone-derived retinoic acid metabolism blocking agents: synthesis and in vitro evaluation with liver microsomal and MCF-7 CYP26A1 cell assays. |
| AID50153 | Evaluation of In vitro antifungal activity against Candida krusei 70 by broth macro dilution method | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20 | Synthesis and antifungal activity of new azole derivatives containing an N-acylmorpholine ring. |
| AID260489 | Opening of large conductance calcium-activated potassium channel in bovine smooth muscle cells at 10 uM | 2006 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 16, Issue:4 | Partial structures of ketoconazole as modulators of the large conductance calcium-activated potassium channel (BK(Ca)). |
| AID477742 | Antimicrobial activity against Candida albicans after 24 hrs | 2010 | European journal of medicinal chemistry, Apr, Volume: 45, Issue:4 | An eco-friendly synthesis and antimicrobial activities of dihydro-2H-benzo- and naphtho-1,3-oxazine derivatives. |
| AID1067047 | Antifungal activity against Cryptococcus neoformans after 72 hrs by micro-broth dilution method | 2014 | European journal of medicinal chemistry, Mar-03, Volume: 74 | Synthesis, antifungal activities and molecular docking studies of novel 2-(2,4-difluorophenyl)-2-hydroxy-3-(1H-1,2,4-triazol-1-yl)propyl dithiocarbamates. |
| AID407020 | Antimicrobial activity against Chk1 deficient Candida albicans CHK21 dissociated biofilms at cell density of 10'3 cells/ml after 48 hrs by XTT assay | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | Role for cell density in antifungal drug resistance in Candida albicans biofilms. |
| AID644181 | Antifungal activity against Penicillium ochrochloron ATCC 9112 after 72 hrs by serial dilution method | 2012 | Bioorganic & medicinal chemistry, Feb-15, Volume: 20, Issue:4 | Synthesis of novel sulfonamide-1,2,4-triazoles, 1,3,4-thiadiazoles and 1,3,4-oxadiazoles, as potential antibacterial and antifungal agents. Biological evaluation and conformational analysis studies. |
| AID294849 | Antifungal activity against Candida parapsilosis ATCC 0306392 after 7 days by micro-broth dilution method | 2007 | European journal of medicinal chemistry, Sep, Volume: 42, Issue:9 | Synthesis of novel triazole derivatives as inhibitors of cytochrome P450 14alpha-demethylase (CYP51). |
| AID1130400 | Antifungal activity against Candida albicans B2630 infected in guinea pig cutaneous candidosis model at 10 mg/kg, po for 14 days measured on day 21 | 1979 | Journal of medicinal chemistry, Aug, Volume: 22, Issue:8 | Antimycotic imidazoles. part 4. Synthesis and antifungal activity of ketoconazole, a new potent orally active broad-spectrum antifungal agent. |
| AID49261 | Tested for minimum subinhibitory concentration against Candida albicans 90 (Candida albicans) at pH 6.5. | 1994 | Journal of medicinal chemistry, Jun-24, Volume: 37, Issue:13 | Derivatives of a novel cyclopeptolide. 1. Synthesis, antifungal activity, and structure-activity relationships. |
| AID49111 | 50% inhibitory activity against Candida albicans (40 clinical isolates) determined at pH-5.8 | 1995 | Journal of medicinal chemistry, Oct-13, Volume: 38, Issue:21 | Antifungal agents. 9. 3-Aryl-4-[alpha-(1H-imidazol-1-yl)arylmethyl]pyrroles: a new class of potent anti-Candida agents. |
| AID678722 | Covalent binding affinity to human liver microsomes assessed per mg of protein at 10 uM after 60 mins presence of NADPH | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
| AID407008 | Antimicrobial activity against fluconazole-resistant Candida albicans FH5 at planktonic cell density of 10'3 cells/ml after 48 hrs by XTT assay | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | Role for cell density in antifungal drug resistance in Candida albicans biofilms. |
| AID1171987 | Antibacterial activity against Klebsiella pneumoniae MTCC 109 assessed as inhibition of visual growth after 24 hrs | 2015 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2 | Facile and diastereoselective synthesis of 3,2'-spiropyrrolidine-oxindoles derivatives, their molecular docking and antiproliferative activities. |
| AID380254 | Antifungal activity against Alternaria alternata by MTT assay | 2006 | Journal of natural products, Dec, Volume: 69, Issue:12 | Bioactive oligostilbenoids from the stem bark of Hopea exalata. |
| AID625280 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID564270 | Antifungal activity against Candida albicans isolate 14 after 48 hrs by broth microdilution method | 2010 | Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9 | A clinical isolate of Candida albicans with mutations in ERG11 (encoding sterol 14alpha-demethylase) and ERG5 (encoding C22 desaturase) is cross resistant to azoles and amphotericin B. |
| AID51046 | Inhibition of Corticoid 11-beta-hydroxylase cytochrome P450 | 1992 | Journal of medicinal chemistry, Jul-24, Volume: 35, Issue:15 | Stereoisomers of ketoconazole: preparation and biological activity. |
| AID53396 | Inhibition of Cytochrome P450 19A1 in Human placental microsomes | 1996 | Journal of medicinal chemistry, Aug-16, Volume: 39, Issue:17 | 3- and 4-pyridylalkyl adamantanecarboxylates: inhibitors of human cytochrome P450(17 alpha) (17 alpha-hydroxylase/C17,20-lyase). Potential nonsteroidal agents for the treatment of prostatic cancer. |
| AID125957 | In vitro evaluation of minimum inhibitory concentration against Microsporum gypseum 22 | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20 | Synthesis and antifungal activity of new azole derivatives containing an N-acylmorpholine ring. |
| AID1474166 | Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index | 2016 | Drug discovery today, Apr, Volume: 21, Issue:4 | DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans. |
| AID73607 | The compound was evaluated for mean zone diameter (inhibition) against filamentous fungi at 1000 ug/mL concentration | 1987 | Journal of medicinal chemistry, Aug, Volume: 30, Issue:8 | Lysosomotropic agents. 7. Broad-spectrum antifungal activity of lysosomotropic detergents. |
| AID511041 | Antimicrobial activity against Curvularia lunata NCIM 716 at 200 ug/disk after 48 hrs by agar disc-diffusion method | 2010 | European journal of medicinal chemistry, Sep, Volume: 45, Issue:9 | Synthesis and bioassay of aminosulfonyl-1,3,4-oxadiazoles and their interconversion to 1,3,4-thiadiazoles. |
| AID313555 | Inhibition of hepatic CYP3A4 at 1 uM | 2008 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 18, Issue:1 | Synthesis, biological evaluation and molecular modelling studies of novel ACD- and ABD-ring steroidomimetics as inhibitors of CYP17. |
| AID1130395 | Antifungal activity against Candida albicans B2630 infected in ovariectomized and hysterectomized Wistar rat vaginal candidosis model at 5 mg/kg, po for 14 days by prophylactic treatment | 1979 | Journal of medicinal chemistry, Aug, Volume: 22, Issue:8 | Antimycotic imidazoles. part 4. Synthesis and antifungal activity of ketoconazole, a new potent orally active broad-spectrum antifungal agent. |
| AID1079939 | Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source] | |||
| AID575108 | Antifungal activity against Madurella mycetomatis isolate 41 by XTT assay | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Madurella mycetomatis is not susceptible to the echinocandin class of antifungal agents. |
| AID262708 | Inhibition of human CYP11B2 expressed in V79 11B2 cells | 2006 | Journal of medicinal chemistry, Apr-06, Volume: 49, Issue:7 | Synthesis and evaluation of heteroaryl-substituted dihydronaphthalenes and indenes: potent and selective inhibitors of aldosterone synthase (CYP11B2) for the treatment of congestive heart failure and myocardial fibrosis. |
| AID405031 | Antifungal activity against Sporothrix schenckii P24223 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by Sensititre YeastOne method | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods. |
| AID635085 | Antifungal activity against Curvularia lunata NCIM 716 after 48 hrs by disk diffusion method | 2012 | European journal of medicinal chemistry, Jan, Volume: 47, Issue:1 | Synthesis, antimicrobial, antimycobacterial and structure-activity relationship of substituted pyrazolo-, isoxazolo-, pyrimido- and mercaptopyrimidocyclohepta[b]indoles. |
| AID323066 | Antifungal activity against Trichophyton mentagrophytes ATCC 9972 by micro-broth dilution method | 2008 | Bioorganic & medicinal chemistry, Jan-15, Volume: 16, Issue:2 | Antifungal and cytotoxic activities of some N-substituted aniline derivatives bearing a hetaryl fragment. |
| AID1472626 | In vitro antifungal activity against Trichophyton mentagrophytes after 7 days by serial dilution method | 2018 | Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1 | Novel Terminal Bipheny-Based Diapophytoene Desaturases (CrtN) Inhibitors as Anti-MRSA/VISR/LRSA Agents with Reduced hERG Activity. |
| AID417962 | Antifungal activity against Cryptococcus neoformans after 48 hrs by broth microdilution technique | 2009 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6 | Relation between lipophilicity of alkyl gallates and antifungal activity against yeasts and filamentous fungi. |
| AID50129 | Evaluation of In vitro antifungal activity against Candida guilliermondii 26 by broth macro dilution method | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20 | Synthesis and antifungal activity of new azole derivatives containing an N-acylmorpholine ring. |
| AID655581 | Antifungal activity against Candida albicans Y0109 after 24 hrs by microbroth dilution method | 2012 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8 | New triazole derivatives as antifungal agents: synthesis via click reaction, in vitro evaluation and molecular docking studies. |
| AID532558 | Antifungal activity against Saccharomyces cerevisiae BY4741 assessed as growth rate at 8 ug/ml (Rvb = 0.144%) | 2008 | Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10 | Differential azole antifungal efficacies contrasted using a Saccharomyces cerevisiae strain humanized for sterol 14 alpha-demethylase at the homologous locus. |
| AID1319260 | Inhibition of CYP3A4 in human liver microsomes using midazolam as substrate assessed as reduction in 1-OH-midazolam formation at 0.04 uM by LC/MS/MS analysis | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18 | Identification of (R)-(2-Chloro-3-(trifluoromethyl)phenyl)(1-(5-fluoropyridin-2-yl)-4-methyl-6,7-dihydro-1H-imidazo[4,5-c]pyridin-5(4H)-yl)methanone (JNJ 54166060), a Small Molecule Antagonist of the P2X7 receptor. |
| AID1263193 | Cytotoxicity against human PC3 cells assessed as growth inhibition at 50 uM | 2015 | Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24 | Synthesis and activity of novel 16-dehydropregnenolone acetate derivatives as inhibitors of type 1 5α-reductase and on cancer cell line SK-LU-1. |
| AID1557076 | Antifungal activity against Candida albicans P-87 assessed as reduction in fungal cell growth incubated for 24 hrs by MTT based broth double dilution method | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Antifungal activity, mode of action variability, and subcellular distribution of coumarin-based antifungal azoles. |
| AID367167 | Cytotoxicity against human A431 cells at 0.001 mg/ml | 2009 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 19, Issue:3 | Synthesis and antifungal activity of 1,2,3-triazole containing fluconazole analogues. |
| AID606212 | Antifungal activity against Candida albicans ATCC Y0109 after 24 hrs by micro-broth dilution method | 2011 | European journal of medicinal chemistry, Jul, Volume: 46, Issue:7 | Design, synthesis and antifungal activities of novel 1,2,4-triazole derivatives. |
| AID625282 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID628511 | Antifungal activity against Candida albicans at 100 ug/ml after 48 hrs by disc diffusion method | 2011 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21 | Synthesis and biological evaluation of some novel triazol-3-ones as antimicrobial agents. |
| AID1328084 | Antifungal activity against Penicillium chrysogenum assessed as inhibition of spore germination at 50 ug/well after 48 hrs by agar well diffusion method | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | Synthesis and antimicrobial activity of styryl/pyrrolyl/pyrazolyl sulfonylmethyl-1,3,4-oxadiazolyl amines and styryl/pyrrolyl/pyrazolyl sulfonylmethyl-1,3,4-thiadiazolyl amines. |
| AID575116 | Antifungal activity against Madurella mycetomatis isolate 55 by XTT assay | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Madurella mycetomatis is not susceptible to the echinocandin class of antifungal agents. |
| AID322165 | Antifungal activity against Candida tropicalis C 137-1997 after 48 hrs by CLSI M27-A2 method | 2008 | Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1 | N-Phenyl and N-phenylalkyl-maleimides acting against Candida spp.: time-to-kill, stability, interaction with maleamic acids. |
| AID244001 | In vitro inhibition of human CYP17 expressed in Escherichia coli incubated with 2.5 uM of substrate progesterone in presence of 2.5 uM of compound | 2005 | Journal of medicinal chemistry, Mar-10, Volume: 48, Issue:5 | Synthesis and evaluation of (pyridylmethylene)tetrahydronaphthalenes/-indanes and structurally modified derivatives: potent and selective inhibitors of aldosterone synthase. |
| AID633965 | Antifungal activity against Candida albicans isolated from human incubated for 72 hrs followed by serial sub-cultivation for 72 hrs by serial dilution technique | 2011 | Bioorganic & medicinal chemistry, Dec-15, Volume: 19, Issue:24 | Novel (E)-1-(4-methyl-2-(alkylamino)thiazol-5-yl)-3-arylprop-2-en-1-ones as potent antimicrobial agents. |
| AID1090142 | Antifungal activity against Cladosporium herbarum assessed as growth inhibition at 23 degC measured after 72 hr | 2005 | Journal of agricultural and food chemistry, Jan-26, Volume: 53, Issue:2 | Antifungal and insect antifeedant 2-phenylethanol esters from the liverwort Balantiopsis cancellata from Chile. |
| AID1130396 | Antifungal activity against Candida albicans B2630 infected in ovariectomized and hysterectomized Wistar rat vaginal candidosis model at 2.5 mg/kg, po for 11 days by prophylactic treatment | 1979 | Journal of medicinal chemistry, Aug, Volume: 22, Issue:8 | Antimycotic imidazoles. part 4. Synthesis and antifungal activity of ketoconazole, a new potent orally active broad-spectrum antifungal agent. |
| AID1467473 | Antifungal activity against Fusarium oxysporum at 100 ug/ml after 48 hrs by agar well diffusion method | 2017 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 27, Issue:14 | Synthesis, SAR and molecular docking studies of benzo[d]thiazole-hydrazones as potential antibacterial and antifungal agents. |
| AID1557081 | Antifungal activity against Candida parapsilosis ATCC 90018 assessed as reduction in fungal cell growth incubated for 24 hrs by MTT based broth double dilution method | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Antifungal activity, mode of action variability, and subcellular distribution of coumarin-based antifungal azoles. |
| AID588218 | FDA HLAED, lactate dehydrogenase (LDH) increase | 2004 | Current drug discovery technologies, Dec, Volume: 1, Issue:4 | Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling. |
| AID1204659 | Antifungal activity against Aspergillus niger assessed as growth inhibition at 0.5 mg/ml after 48 hrs by well diffusion method | 2015 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 25, Issue:12 | Isolation, semi-synthesis and bio-evaluation of spatane derivatives from the brown algae Stoechospermum marginatum. |
| AID532528 | Antifungal activity against Saccharomyces cerevisiae BY4741 harboring human CYP51 assessed as growth rate at 2 ug/ml (Rvb = 0.157%) | 2008 | Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10 | Differential azole antifungal efficacies contrasted using a Saccharomyces cerevisiae strain humanized for sterol 14 alpha-demethylase at the homologous locus. |
| AID488642 | Antimicrobial activity against Candida parapsilosis ATCC 22019 by broth dilution method | 2010 | Journal of natural products, Jun-25, Volume: 73, Issue:6 | Alkaloids from the bark of Guatteria hispida and their evaluation as antioxidant and antimicrobial agents. |
| AID1473740 | Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1 | A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
| AID364749 | Inhibition of human recombinant CYP17 expressed in Escherichia coli pJL17/OR | 2008 | Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19 | Novel aldosterone synthase inhibitors with extended carbocyclic skeleton by a combined ligand-based and structure-based drug design approach. |
| AID1456578 | Antifungal activity against Candida parapsilosis isolate 22019 by micro-broth dilution method | 2017 | Bioorganic & medicinal chemistry letters, 05-15, Volume: 27, Issue:10 | Design, synthesis, and in vitro evaluation of novel antifungal triazoles. |
| AID363974 | Antimicrobial activity against Cryptococcus neoformans IM 052470 isolate at 6.25 ug/ml after 48 hrs | 2008 | Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17 | In vitro antifungal activity of polyfunctionalized 2-(hetero)arylquinolines prepared through imino Diels-Alder reactions. |
| AID55036 | In vitro antifungal activity against human pathogenic fungi, Cryptococcus neoformans | 2000 | Bioorganic & medicinal chemistry letters, Apr-17, Volume: 10, Issue:8 | Suitably functionalised pyrimidines as potential antimycotic agents. |
| AID1319262 | Inhibition of CYP3A4 in human liver microsomes using midazolam as substrate assessed as reduction in 1-OH-midazolam formation at 0.16 uM by LC/MS/MS analysis | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18 | Identification of (R)-(2-Chloro-3-(trifluoromethyl)phenyl)(1-(5-fluoropyridin-2-yl)-4-methyl-6,7-dihydro-1H-imidazo[4,5-c]pyridin-5(4H)-yl)methanone (JNJ 54166060), a Small Molecule Antagonist of the P2X7 receptor. |
| AID395656 | Antifungal activity against Candida albicans ATCC 10231 assessed as growth inhibition at 200 uM after 24 hrs | 2009 | European journal of medicinal chemistry, Jan, Volume: 44, Issue:1 | Penetratin and derivatives acting as antifungal agents. |
| AID214268 | In vitro evaluation of minimum inhibitory concentration against Trichophyton mentagrophytes 23 | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20 | Synthesis and antifungal activity of new azole derivatives containing an N-acylmorpholine ring. |
| AID486242 | Antifungal activity against Trichophyton rubrum C 113 after 48 hrs | 2010 | European journal of medicinal chemistry, Jun, Volume: 45, Issue:6 | Naftifine-analogues as anti-Trypanosoma cruzi agents. |
| AID588214 | FDA HLAED, liver enzyme composite activity | 2004 | Current drug discovery technologies, Dec, Volume: 1, Issue:4 | Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling. |
| AID380258 | Antifungal activity against Pyricularia oryzae by MTT assay | 2006 | Journal of natural products, Dec, Volume: 69, Issue:12 | Bioactive oligostilbenoids from the stem bark of Hopea exalata. |
| AID425722 | Antimicrobial activity against Balamuthia mandrillaris ATCC 50209 infected in HBMEC assessed as inhibition of amoeba-induced cytopathogenicity at 5 ug/mL after 24 hrs by LDH release assay | 2007 | Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12 | Effect of antimicrobial compounds on Balamuthia mandrillaris encystment and human brain microvascular endothelial cell cytopathogenicity. |
| AID530959 | Antifungal activity against Cryptococcus neoformans ATCC 90113 after 72 hrs by CLSI method | 2008 | Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7 | Potent in vitro antifungal activities of naturally occurring acetylenic acids. |
| AID1209972 | Inhibition of CYP2C19 in human liver microsomes using S-mephenytoin as substrate after 8 mins by LC-MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5 | Identifying a selective substrate and inhibitor pair for the evaluation of CYP2J2 activity. |
| AID515181 | Antimicrobial activity against Candida albicans CGMCC 2.2086 after 48 hrs by modified microdilution method | 2010 | European journal of medicinal chemistry, Oct, Volume: 45, Issue:10 | Synthesis and antimicrobial activities of novel 1H-dibenzo[a,c]carbazoles from dehydroabietic acid. |
| AID599149 | Antibacterial activity against Staphylococcus aureus after 24 hrs by MTT assay | 2008 | European journal of medicinal chemistry, Mar, Volume: 43, Issue:3 | Synthesis, crystal structure and antimicrobial activity of deoxybenzoin derivatives from genistein. |
| AID1079931 | Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source] | |||
| AID768393 | Antifungal activity against Candida albicans MTCC 227 by conventional broth microdilution method | 2013 | European journal of medicinal chemistry, Sep, Volume: 67 | Synthesis, antimicrobial and cytotoxic activities of some novel thiazole clubbed 1,3,4-oxadiazoles. |
| AID1456576 | Antifungal activity against Candida albicans isolate Y0109 by micro-broth dilution method | 2017 | Bioorganic & medicinal chemistry letters, 05-15, Volume: 27, Issue:10 | Design, synthesis, and in vitro evaluation of novel antifungal triazoles. |
| AID55175 | Minimum inhibitory concentration against Cryptococcus neoformans | 2004 | Bioorganic & medicinal chemistry letters, Jan-19, Volume: 14, Issue:2 | Synthesis of galactopyranosyl amino alcohols as a new class of antitubercular and antifungal agents. |
| AID525140 | Antifungal activity against Fusarium moniliforme clade 2 by microdilution method | 2008 | Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6 | In vitro antifungal susceptibility and molecular characterization of clinical isolates of Fusarium verticillioides (F. moniliforme) and Fusarium thapsinum. |
| AID73610 | The compound was evaluated for mean zone diameter (inhibition) against filamentous fungi at 500 ug/mL concentration | 1987 | Journal of medicinal chemistry, Aug, Volume: 30, Issue:8 | Lysosomotropic agents. 7. Broad-spectrum antifungal activity of lysosomotropic detergents. |
| AID633962 | Antifungal activity against Penicillium funiculosum ATCC 36839 incubated for 72 hrs followed by serial sub-cultivation for 72 hrs by serial dilution technique | 2011 | Bioorganic & medicinal chemistry, Dec-15, Volume: 19, Issue:24 | Novel (E)-1-(4-methyl-2-(alkylamino)thiazol-5-yl)-3-arylprop-2-en-1-ones as potent antimicrobial agents. |
| AID447225 | Antifungal activity against Kluyveromyces fragilis NRRL 2415 at 20 ug after 72 hrs by agar disk diffusion assay | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11 | Synthesis, Raman, FT-IR, NMR spectroscopic characterization, antimicrobial activity, cytotoxicity and DNA binding of new mixed aza-oxo-thia macrocyclic compounds. |
| AID1166505 | Displacement of [3H]MIB from rat prostate cytosol androgen receptor at 1x10'-10 to 1x10'-7 M relative to control | 2014 | Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21 | Effect of dehydroepiandrosterone derivatives on the activity of 5α-reductase isoenzymes and on cancer cell line PC-3. |
| AID640968 | Antifungal activity against Aspergillus oryzae NCIM 643 after 48 hrs by agar well diffusion assay | 2012 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2 | Synthesis, characterization and in vitro biological evaluation of some novel diarylsulfonylureas as potential cytotoxic and antimicrobial agents. |
| AID150751 | Inhibition of P-glycoprotein using ATPase in MDR1 membranes | 2003 | Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9 | Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery. |
| AID363754 | Antimicrobial activity against Candida glabrata C115 isolate at 6.25 ug/ml after 24 hrs | 2008 | Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17 | In vitro antifungal activity of polyfunctionalized 2-(hetero)arylquinolines prepared through imino Diels-Alder reactions. |
| AID79311 | Number of skin sections yielding negative culture / total (48) (percentage) in guinea pig dermatophytosis at dose of 40 mg/kg was determined in vitro. (Value is from Six skin sections cut out from each treated site) | 1987 | Journal of medicinal chemistry, Jun, Volume: 30, Issue:6 | Synthesis and oral antifungal activity of novel azolylpropanolones and related compounds. |
| AID1481507 | Inhibition of CYP3A4 in rat liver microsomes assessed as 6beta-hydroxytestosterone formation using testosterone as substrate by reverse-phase HPLC analysis | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Exploration of 2-((Pyridin-4-ylmethyl)amino)nicotinamide Derivatives as Potent Reversal Agents against P-Glycoprotein-Mediated Multidrug Resistance. |
| AID1481915 | Inhibition of CYP3A4 in rat liver microsomes assessed as decrease in 6beta-OH testosterone levels using testosterone as substrate by HPLC analysis | 2017 | Journal of medicinal chemistry, 04-27, Volume: 60, Issue:8 | Design, Synthesis, and Pharmacological Characterization of N-(4-(2 (6,7-Dimethoxy-3,4-dihydroisoquinolin-2(1H)yl)ethyl)phenyl)quinazolin-4-amine Derivatives: Novel Inhibitors Reversing P-Glycoprotein-Mediated Multidrug Resistance. |
| AID633955 | Antifungal activity against Penicillium ochrochloron ATCC 9112 after 72 hrs by serial dilution technique | 2011 | Bioorganic & medicinal chemistry, Dec-15, Volume: 19, Issue:24 | Novel (E)-1-(4-methyl-2-(alkylamino)thiazol-5-yl)-3-arylprop-2-en-1-ones as potent antimicrobial agents. |
| AID420215 | Antimicrobial activity against Enterococcus faecalis UFPEDA 138 after 20 hrs by twofold serial dilution technique | 2009 | European journal of medicinal chemistry, May, Volume: 44, Issue:5 | Synthesis, antimicrobial and cytotoxic activities of some 5-arylidene-4-thioxo-thiazolidine-2-ones. |
| AID1437344 | Inhibition of CYP3A4 using in human liver microsomes using testosterone as substrate after 5 to 15 mins | |||
| AID211473 | In vitro evaluation of minimum inhibitory concentration against Torulopsis glabrata 78 | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20 | Synthesis and antifungal activity of new azole derivatives containing an N-acylmorpholine ring. |
| AID1312609 | Antifungal activity against naftifine-sensitive Trichophyton mentagrophytes after 7 days by serial dilution method | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10 | Discovery of Benzocycloalkane Derivatives Efficiently Blocking Bacterial Virulence for the Treatment of Methicillin-Resistant S. aureus (MRSA) Infections by Targeting Diapophytoene Desaturase (CrtN). |
| AID397172 | Antifungal activity against Aspergillus flavus PTCC 5003 after 48 hrs by microplate alamar blue assay | 2009 | European journal of medicinal chemistry, May, Volume: 44, Issue:5 | Synthesis, antimicrobial evaluation and QSAR study of some 3-hydroxypyridine-4-one and 3-hydroxypyran-4-one derivatives. |
| AID1557090 | Cytotoxicity against human HepG2 cells assessed as reduction in cell viability at 5 to 50 uM incubated for 24 hrs by XTT assay | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Antifungal activity, mode of action variability, and subcellular distribution of coumarin-based antifungal azoles. |
| AID664301 | Antifungal activity against Aspergillus fumigatus MTCC 343 at 100 ug/disc by paper disc diffusion technique | 2012 | European journal of medicinal chemistry, Jul, Volume: 53 | Synthesis of benzimidazolyl-1,3,4-oxadiazol-2ylthio-N-phenyl (benzothiazolyl) acetamides as antibacterial, antifungal and antituberculosis agents. |
| AID205563 | Minimum inhibitory concentration against Staphylococcus aureus ATCC 29213 by agar plate dilution method; NT=Not tested | 2004 | Bioorganic & medicinal chemistry letters, Feb-09, Volume: 14, Issue:3 | Synthesis and antifungal activities of phenylenedithioureas. |
| AID565892 | Metabolic stability in rat liver microsomes in presence of non-selective cytochrome P450 inhibitor ketoconazole | 2011 | European journal of medicinal chemistry, Jan, Volume: 46, Issue:1 | CYP1A2-mediated biotransformation of cardioactive 2-thienylidene-3,4-methylenedioxybenzoylhydrazine (LASSBio-294) by rat liver microsomes and human recombinant CYP enzymes. |
| AID419397 | Antifungal activity against Aspergillus fumigatus ATCC 46645 after 48 hrs by agar streak dilution method | 2009 | European journal of medicinal chemistry, May, Volume: 44, Issue:5 | Synthesis and anti-microbial screening of some Schiff bases of 3-amino-6,8-dibromo-2-phenylquinazolin-4(3H)-ones. |
| AID524795 | Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay | 2009 | Nature chemical biology, Oct, Volume: 5, Issue:10 | Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum. |
| AID554714 | Antimicrobial activity against Candida krusei NZCDC 89.102 after 48 hrs by CLSI method | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2 | Abc1p is a multidrug efflux transporter that tips the balance in favor of innate azole resistance in Candida krusei. |
| AID494004 | Antifungal activity against Cryptococcus neoformans ATCC 32264 assessed as inhibition of fungal growth at 100 uM | 2010 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 20, Issue:16 | New antifungal peptides. Synthesis, bioassays and initial structure prediction by CD spectroscopy. |
| AID48796 | In vitro minimum inhibitory concentration of compound was determined against Candida tropicalis after 48 hr | 2000 | Bioorganic & medicinal chemistry letters, Aug-21, Volume: 10, Issue:16 | 3-Phenyl-5-methyl-2H,5H-furan-2-ones: tuning antifungal activity by varying substituents on the phenyl ring. |
| AID1319268 | Inhibition of CYP3A4 in human liver microsomes using midazolam as substrate assessed as reduction in 4-OH-midazolam formation at 0.16 uM by LC/MS/MS analysis | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18 | Identification of (R)-(2-Chloro-3-(trifluoromethyl)phenyl)(1-(5-fluoropyridin-2-yl)-4-methyl-6,7-dihydro-1H-imidazo[4,5-c]pyridin-5(4H)-yl)methanone (JNJ 54166060), a Small Molecule Antagonist of the P2X7 receptor. |
| AID596445 | Antifungal activity against Saccharomyces cerevisiae ATCC 9763 | 2011 | Bioorganic & medicinal chemistry, May-01, Volume: 19, Issue:9 | Antifungal, cytotoxic and SAR studies of a series of N-alkyl, N-aryl and N-alkylphenyl-1,4-pyrrolediones and related compounds. |
| AID555821 | Ratio of MIC50 for Candida albicans 5674 to MIC50 for cdr1/cdr1 deficient Candida albicans STY19 | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | Relative contributions of the Candida albicans ABC transporters Cdr1p and Cdr2p to clinical azole resistance. |
| AID553066 | Inhibition of human CYP11B2 expressed in hamster V79MZ cells using 11-deoxycorticosterone substrate | 2011 | ACS medicinal chemistry letters, Jan-13, Volume: 2, Issue:1 | First Selective CYP11B1 Inhibitors for the Treatment of Cortisol-Dependent Diseases. |
| AID688636 | Antifungal activity against Penicillium chrysogenum at 50 ug after 48 hrs by agar well diffusion method | 2011 | European journal of medicinal chemistry, Nov, Volume: 46, Issue:11 | Synthesis and antimicrobial activity of amido linked pyrrolyl and pyrazolyl-oxazoles, thiazoles and imidazoles. |
| AID382513 | Antifungal activity against Candida albicans isolate by broth dilution antifungal susceptibility test | 2008 | European journal of medicinal chemistry, Jan, Volume: 43, Issue:1 | New triazole and triazolothiadiazine derivatives as possible antimicrobial agents. |
| AID635084 | Antifungal activity against Fusarium solani NCIM 1330 after 48 hrs by disk diffusion method | 2012 | European journal of medicinal chemistry, Jan, Volume: 47, Issue:1 | Synthesis, antimicrobial, antimycobacterial and structure-activity relationship of substituted pyrazolo-, isoxazolo-, pyrimido- and mercaptopyrimidocyclohepta[b]indoles. |
| AID564265 | Effect on sterol composition in Candida albicans isolate 14 expressing wild type erg11 and erg5 assessed as obtusifoliol level after 2 hrs by gas chromatography | 2010 | Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9 | A clinical isolate of Candida albicans with mutations in ERG11 (encoding sterol 14alpha-demethylase) and ERG5 (encoding C22 desaturase) is cross resistant to azoles and amphotericin B. |
| AID1557083 | Antifungal activity against Candida guilliermondii T-47 assessed as reduction in fungal cell growth incubated for 24 hrs by MTT based broth double dilution method | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Antifungal activity, mode of action variability, and subcellular distribution of coumarin-based antifungal azoles. |
| AID1435415 | Anti-bacterial activity against methicillin-resistant Staphylococcus aureus ATCC 700699 measured after 24 hrs by microtiter broth dilution method | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Design, synthesis and antimicrobial evaluation of novel benzoxazole derivatives. |
| AID242795 | In vitro inhibitory concentration against human CYP11B2 expressed in V79MZh hamster fibroblasts incubated with 100 nM of substrate deoxy-corticosterone in presence of the compound | 2005 | Journal of medicinal chemistry, Mar-10, Volume: 48, Issue:5 | Synthesis and evaluation of (pyridylmethylene)tetrahydronaphthalenes/-indanes and structurally modified derivatives: potent and selective inhibitors of aldosterone synthase. |
| AID1079932 | Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source] | |||
| AID625288 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID750213 | Antifungal activity against Candida albicans NRRLY-477 assessed as diameter of inhibition zone at 0.5 mg/ml after 24 hrs by agar well diffusion method | 2013 | European journal of medicinal chemistry, Jun, Volume: 64 | Thiourea derivatives incorporating a hippuric acid moiety: synthesis and evaluation of antibacterial and antifungal activities. |
| AID1104304 | Antifungal activity against Hypocrea rufa IAM 5061 at 28 degC measured after 72 hr by microdilution method | 2010 | Chemical & pharmaceutical bulletin, Feb, Volume: 58, Issue:2 | Sulfonamide-1,2,4-thiadiazole derivatives as antifungal and antibacterial agents: synthesis, biological evaluation, lipophilicity, and conformational studies. |
| AID420666 | Antifungal activity against Microsporum gypseum by micro-broth dilution method | 2009 | European journal of medicinal chemistry, May, Volume: 44, Issue:5 | Design, synthesis, and biological evaluation of novel triazole derivatives as inhibitors of cytochrome P450 14alpha-demethylase. |
| AID515013 | Antifungal activity against Trichophyton rubrum by micro-broth dilution method | 2010 | European journal of medicinal chemistry, Oct, Volume: 45, Issue:10 | Synthesis and antifungal evaluation of novel triazole derivatives as inhibitors of cytochrome P450 14alpha-demethylase. |
| AID48050 | Minimum inhibitory concentration against Candida parapsilosis | 2004 | Bioorganic & medicinal chemistry letters, Jan-19, Volume: 14, Issue:2 | Synthesis of galactopyranosyl amino alcohols as a new class of antitubercular and antifungal agents. |
| AID405013 | Antifungal activity against Sporothrix schenckii PSSA81 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by Sensititre YeastOne method | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods. |
| AID363779 | Antimicrobial activity against Cryptococcus neoformans IM 983040 isolate at 6.25 ug/ml after 48 hrs | 2008 | Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17 | In vitro antifungal activity of polyfunctionalized 2-(hetero)arylquinolines prepared through imino Diels-Alder reactions. |
| AID48793 | In vitro evaluation of minimum inhibitory concentration against Candida tropicalis 2.11 | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20 | Synthesis and antifungal activity of new azole derivatives containing an N-acylmorpholine ring. |
| AID1130379 | Antifungal activity against Candida albicans assessed as growth inhibition in sabouraud broth after 14 days | 1979 | Journal of medicinal chemistry, Aug, Volume: 22, Issue:8 | Antimycotic imidazoles. part 4. Synthesis and antifungal activity of ketoconazole, a new potent orally active broad-spectrum antifungal agent. |
| AID765039 | Antifungal activity against Candida albicans ATCC 10231 by MTT assay | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17 | 3-Aryl-4-acyloxyethoxyfuran-2(5H)-ones as inhibitors of tyrosyl-tRNA synthetase: synthesis, molecular docking and antibacterial evaluation. |
| AID636991 | Antifungal activity against Aspergillus fumigatus after 48 hrs by agar streak dilution method | 2012 | European journal of medicinal chemistry, Feb, Volume: 48 | Synthesis and biological evaluation of some thiazolidinones as antimicrobial agents. |
| AID687504 | Antifungal activity against Aspergillus fumigatus ATCC 26934 by NCCLS broth microdilution method | 2012 | Bioorganic & medicinal chemistry, Oct-15, Volume: 20, Issue:20 | Structure-activity relationship study of nitrosopyrimidines acting as antifungal agents. |
| AID632563 | Antibacterial activity against Escherichia coli at 200 ug/mL after 24 hrs by agar cup diffusion method | 2011 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 21, Issue:24 | A new antifungal briarane diterpenoid from the gorgonian Junceella juncea Pallas. |
| AID334245 | Antimicrobial activity against Pseudomonas aeruginosa NCIMB 10421 after 24 hrs by microdilution technique | 2002 | Journal of natural products, Apr, Volume: 65, Issue:4 | Antimicrobial activities of a new schizozygane indoline alkaloid from Schizozygia coffaeoides and the revised structure of isoschizogaline. |
| AID633912 | Antifungal activity against Aspergillus niger ATCC 16404 at 10 ug/mL after 72 hrs by agar cup plate method | 2012 | European journal of medicinal chemistry, Jan, Volume: 47, Issue:1 | Isoxazoles incorporated N-substituted decahydroquinolines: a precursor to the next generation antimicrobial drug. |
| AID463561 | Inhibition of human recombinant aromatase at 1 uM | 2010 | Journal of natural products, Feb-26, Volume: 73, Issue:2 | The taiwaniaquinoids: a review. |
| AID112513 | In vivo activity against subacute systemic murine candidiasis in mice at a daose of 12.5-100 mg/kg dosage range. Value was determined at day 15 after infection | 1987 | Journal of medicinal chemistry, Jun, Volume: 30, Issue:6 | Synthesis and oral antifungal activity of novel azolylpropanolones and related compounds. |
| AID1467471 | Antifungal activity against Fusarium oxysporum at 50 ug/ml after 48 hrs by agar well diffusion method | 2017 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 27, Issue:14 | Synthesis, SAR and molecular docking studies of benzo[d]thiazole-hydrazones as potential antibacterial and antifungal agents. |
| AID42884 | Inhibition of Candida parapsilosis ATCC 22019 growth for 24 hours in vitro. | 2001 | Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17 | 3-Phenyl-5-acyloxymethyl-2H,5H-furan-2-ones: synthesis and biological activity of a novel group of potential antifungal drugs. |
| AID681119 | TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1a-expressing LLC-PK1 cells | 2003 | Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9 | Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery. |
| AID1068779 | Antifungal activity against Penicillium chrysogenum at 100 ug/well after 48 hrs by agar well diffusion method | 2014 | European journal of medicinal chemistry, Feb-12, Volume: 73 | Synthesis and antimicrobial activity of (1,4-phenylene)bis(arylsulfonylpyrazoles and isoxazoles). |
| AID530943 | Antifungal activity against Candida parapsilosis ATCC 22019 at 9.4 uM after 48 hrs by CLSI method | 2008 | Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7 | Potent in vitro antifungal activities of naturally occurring acetylenic acids. |
| AID1160914 | Inhibition of mouse CYP27B1 using 1,25(OH)2D3 substrate in presence of bovine adrenodoxin, adrenodoxin reductase and NADPH incubated at 37 degC for 25 mins by HPLC method | 2014 | Journal of medicinal chemistry, Sep-25, Volume: 57, Issue:18 | Small-molecule inhibitors of 25-hydroxyvitamin D-24-hydroxylase (CYP24A1): synthesis and biological evaluation. |
| AID1221963 | Transporter substrate index ratio of permeability from apical to basolateral side in human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY335979 | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2 | Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
| AID362915 | Antifungal activity against Penicillium notatum after 24 hrs by broth microdilution method | 2008 | Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17 | NO-donors. Part 17: Synthesis and antimicrobial activity of novel ketoconazole-NO-donor hybrid compounds. |
| AID449695 | Antifungal activity against Curvularia lunata NCIM 716 after 48 hrs by microdilution susceptibility method | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11 | Synthesis, antimicrobial and antioxidant activities of substituted pyrazoles, isoxazoles, pyrimidine and thioxopyrimidine derivatives. |
| AID723710 | Antifungal activity against Penicillium ochrochloron ATCC 9112 after 72 hrs by serial dilution technique | 2013 | Bioorganic & medicinal chemistry, Jan-15, Volume: 21, Issue:2 | Synthesis and biological evaluation of some 5-arylidene-2-(1,3-thiazol-2-ylimino)-1,3-thiazolidin-4-ones as dual anti-inflammatory/antimicrobial agents. |
| AID1268949 | Inhibition of CYP3A4 (unknown origin) up to 10 uM | 2016 | Bioorganic & medicinal chemistry, Jan-15, Volume: 24, Issue:2 | Chlorophenoxy aminoalkyl derivatives as histamine H(3)R ligands and antiseizure agents. |
| AID666780 | Antifungal activity against Microbotryum violaceum at 0.05 mg by agar diffusion test | 2012 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 22, Issue:13 | Bioactive briarane diterpenoids from the South China Sea gorgonian Dichotella gemmacea. |
| AID574249 | Antifungal activity against 10'7 cells/ml wild-type Candida albicans BF-1 planktonic cells by XTT reduction assay | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | Cell density and cell aging as factors modulating antifungal resistance of Candida albicans biofilms. |
| AID1204661 | Antifungal activity against Aspergillus terreus assessed as growth inhibition at 0.5 mg/ml after 48 hrs by well diffusion method | 2015 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 25, Issue:12 | Isolation, semi-synthesis and bio-evaluation of spatane derivatives from the brown algae Stoechospermum marginatum. |
| AID340949 | Antifungal activity against Candida albicans isolates from HIV infected patient before fluconazole therapy by NCCLS M27-A2 method | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8 | Cross-resistance to medical and agricultural azole drugs in yeasts from the oropharynx of human immunodeficiency virus patients and from environmental Bavarian vine grapes. |
| AID519286 | Antifungal activity against Candida parapsilosis ATCC 22019 by WIDERYST method | 2008 | Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3 | Reliability of the WIDERYST susceptibility testing system for detection of in vitro antifungal resistance in yeasts. |
| AID376050 | Antifungal activity against Saccharomyces cerevisiae ATCC 9763 by agar dilution method | 1999 | Journal of natural products, Oct, Volume: 62, Issue:10 | In vitro evaluation of antifungal properties of phenylpropanoids and related compounds acting against dermatophytes. |
| AID774146 | Inhibition of CYP1A2 in human liver microsomes assessed as phenacetin demethylation to acetaminophen at 1 uM after 10 mins relative to control | 2013 | Journal of medicinal chemistry, Oct-10, Volume: 56, Issue:19 | Rational development of 4-aminopyridyl-based inhibitors targeting Trypanosoma cruzi CYP51 as anti-chagas agents. |
| AID1319267 | Inhibition of CYP3A4 in human liver microsomes using midazolam as substrate assessed as reduction in 4-OH-midazolam formation at 0.08 uM by LC/MS/MS analysis | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18 | Identification of (R)-(2-Chloro-3-(trifluoromethyl)phenyl)(1-(5-fluoropyridin-2-yl)-4-methyl-6,7-dihydro-1H-imidazo[4,5-c]pyridin-5(4H)-yl)methanone (JNJ 54166060), a Small Molecule Antagonist of the P2X7 receptor. |
| AID644180 | Antifungal activity against Penicillium funiculosum ATCC 36839 after 72 hrs by serial dilution method | 2012 | Bioorganic & medicinal chemistry, Feb-15, Volume: 20, Issue:4 | Synthesis of novel sulfonamide-1,2,4-triazoles, 1,3,4-thiadiazoles and 1,3,4-oxadiazoles, as potential antibacterial and antifungal agents. Biological evaluation and conformational analysis studies. |
| AID582801 | Antifungal activity against Candida albicans isolate 490 harboring ERG3 D147G, T330A, A351V and ERG11 F72S, T229A, E266D, N440S, V488I, R523G mutant genes by broth microdilution method | 2010 | Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11 | Identification and characterization of four azole-resistant erg3 mutants of Candida albicans. |
| AID1557095 | Cytotoxicity against human HEK293T cells assessed as reduction in cell viability at 5 to 50 uM incubated for 24 hrs by XTT assay relative to control | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Antifungal activity, mode of action variability, and subcellular distribution of coumarin-based antifungal azoles. |
| AID19468 | Partition coefficient (logP) | 2003 | Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9 | Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery. |
| AID53207 | Inhibition of cholesterol side chain cleavage cytochrome P450 | 1992 | Journal of medicinal chemistry, Jul-24, Volume: 35, Issue:15 | Stereoisomers of ketoconazole: preparation and biological activity. |
| AID554716 | Antimicrobial activity against Candida krusei NZCDC 90.147 after 48 hrs by CLSI method | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2 | Abc1p is a multidrug efflux transporter that tips the balance in favor of innate azole resistance in Candida krusei. |
| AID330520 | Toxicity against human HepG2 cells at 6.25 ug/ml in presence of merine microbial F10104 extract | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Mar-13, Volume: 104, Issue:11 | High-throughput synergy screening identifies microbial metabolites as combination agents for the treatment of fungal infections. |
| AID340017 | Inhibition of CYP3A4 in human liver microsome | 2008 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14 | Synthesis of novel ketoconazole derivatives as inhibitors of the human Pregnane X Receptor (PXR; NR1I2; also termed SXR, PAR). |
| AID1110742 | Antifungal activity against Pichia kudriavzevii E 28 after 24 hr by microdilution broth method | 2002 | Farmaco (Societa chimica italiana : 1989), Feb, Volume: 57, Issue:2 | Ring substituted 3-phenyl-1-(2-pyrazinyl)-2-propen-1-ones as potential photosynthesis-inhibiting, antifungal and antimycobacterial agents. |
| AID420217 | Antimicrobial activity against Candida albicans UFPEDA 1007 after 48 hrs by twofold serial dilution technique | 2009 | European journal of medicinal chemistry, May, Volume: 44, Issue:5 | Synthesis, antimicrobial and cytotoxic activities of some 5-arylidene-4-thioxo-thiazolidine-2-ones. |
| AID303380 | Antitrypanosomal activity against Trypanosoma cruzi Y | 2007 | Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24 | In vivo anti-Chagas vinylthio-, vinylsulfinyl-, and vinylsulfonylbenzofuroxan derivatives. |
| AID572708 | Binding affinity to bovine CYP51 | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | Identification, characterization, and azole-binding properties of Mycobacterium smegmatis CYP164A2, a homolog of ML2088, the sole cytochrome P450 gene of Mycobacterium leprae. |
| AID1130383 | Antifungal activity against Phialophora verrucosa assessed as growth inhibition in sabouraud broth after 14 days | 1979 | Journal of medicinal chemistry, Aug, Volume: 22, Issue:8 | Antimycotic imidazoles. part 4. Synthesis and antifungal activity of ketoconazole, a new potent orally active broad-spectrum antifungal agent. |
| AID594132 | Antimicrobial activity against Staphylococcus aureus ATCC 29213 after 24 hrs by agar well diffusion method | 2011 | European journal of medicinal chemistry, May, Volume: 46, Issue:5 | Synthesis, antimicrobial, antioxidant, anti-hemolytic and cytotoxic evaluation of new imidazole-based heterocycles. |
| AID1254878 | Inhibition of CYP3A4 (unknown origin) using luciferin tagged substrate preincubated for 10 mins before substrate addition | 2015 | European journal of medicinal chemistry, Oct-20, Volume: 103 | Discovery of potent and selective cytotoxic activity of new quinazoline-ureas against TMZ-resistant glioblastoma multiforme (GBM). |
| AID84879 | The compound was tested for the inhibition of all-trans retinoic acid (ATRA) catabolism using 7.27 pmol [11,12-3H]-ATRA as substrate in microsomal preparations of male hamster liver fortified with NADPH | 2000 | Bioorganic & medicinal chemistry letters, Sep-04, Volume: 10, Issue:17 | Potent inhibition of retinoic acid metabolism enzyme(s) by novel azolyl retinoids. |
| AID262553 | Antifungal activity against Sporothrix schenckii | 2006 | Journal of medicinal chemistry, Apr-20, Volume: 49, Issue:8 | Structure-based optimization of azole antifungal agents by CoMFA, CoMSIA, and molecular docking. |
| AID515010 | Antifungal activity against Cryptococcus neoformans after 72 hrs by micro-broth dilution method | 2010 | European journal of medicinal chemistry, Oct, Volume: 45, Issue:10 | Synthesis and antifungal evaluation of novel triazole derivatives as inhibitors of cytochrome P450 14alpha-demethylase. |
| AID49127 | Tested In vitro for antifungal activity at pH 5.8 | 2002 | Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13 | Antifungal agents. 10. New derivatives of 1-[(aryl)[4-aryl-1H-pyrrol-3-yl]methyl]-1H-imidazole, synthesis, anti-candida activity, and quantitative structure-analysis relationship studies. |
| AID1319258 | Inhibition of CYP3A4 in human liver microsomes using midazolam as substrate assessed as reduction in 1-OH-midazolam formation at 0.01 uM by LC/MS/MS analysis | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18 | Identification of (R)-(2-Chloro-3-(trifluoromethyl)phenyl)(1-(5-fluoropyridin-2-yl)-4-methyl-6,7-dihydro-1H-imidazo[4,5-c]pyridin-5(4H)-yl)methanone (JNJ 54166060), a Small Molecule Antagonist of the P2X7 receptor. |
| AID420216 | Antimicrobial activity against Mycobacterium smegmatis UFPEDA 71 after 20 hrs by twofold serial dilution technique | 2009 | European journal of medicinal chemistry, May, Volume: 44, Issue:5 | Synthesis, antimicrobial and cytotoxic activities of some 5-arylidene-4-thioxo-thiazolidine-2-ones. |
| AID454782 | Antifungal activity against Trichophyton mentagrophytes ATCC 9972 after 48 hrs by broth microdilution technique | 2009 | Bioorganic & medicinal chemistry, Nov-01, Volume: 17, Issue:21 | 5-Nitrofuranes and 5-nitrothiophenes with anti-Trypanosoma cruzi activity and ability to accumulate squalene. |
| AID633957 | Antifungal activity against Candida albicans isolated from human after 72 hrs by serial dilution technique | 2011 | Bioorganic & medicinal chemistry, Dec-15, Volume: 19, Issue:24 | Novel (E)-1-(4-methyl-2-(alkylamino)thiazol-5-yl)-3-arylprop-2-en-1-ones as potent antimicrobial agents. |
| AID738374 | Inhibition of human CYP3A4 at 10 uM | 2013 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 23, Issue:7 | Synthesis and evaluation of non-dimeric HCV NS5A inhibitors. |
| AID687549 | Antifungal activity against Microsporum gypseum CCC 115 by NCCLS broth microdilution method | 2012 | Bioorganic & medicinal chemistry, Oct-15, Volume: 20, Issue:20 | Structure-activity relationship study of nitrosopyrimidines acting as antifungal agents. |
| AID207275 | Inhibition of rat testicular Steroid 17-alpha-hydroxylase/17,20 lyase | 1995 | Journal of medicinal chemistry, Oct-13, Volume: 38, Issue:21 | Esters of 3-pyridylacetic acid that combine potent inhibition of 17 alpha-hydroxylase/C17,20-lyase (cytochrome P45017 alpha) with resistance to esterase hydrolysis. |
| AID532551 | Antifungal activity against Saccharomyces cerevisiae BY4741 harboring human CYP51 assessed as growth rate at 8 ug/ml (Rvb = 0.157%) | 2008 | Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10 | Differential azole antifungal efficacies contrasted using a Saccharomyces cerevisiae strain humanized for sterol 14 alpha-demethylase at the homologous locus. |
| AID655586 | Antifungal activity against Trichophyton rubrum by microbroth dilution method | 2012 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8 | New triazole derivatives as antifungal agents: synthesis via click reaction, in vitro evaluation and molecular docking studies. |
| AID228082 | In vivo activity against vaginal candidoses in rats, measured as the ratio of animals cured/animals infected (C/I) at dose 1.25 mg/kg; 0/12 | 1984 | Journal of medicinal chemistry, Jul, Volume: 27, Issue:7 | Antimycotic azoles. 7. Synthesis and antifungal properties of a series of novel triazol-3-ones. |
| AID448518 | Antimicrobial activity against Aspergillus niger after 24 hrs by serial dilution method | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11 | Synthesis of some novel pyrazolo[3,4-b]pyridine and pyrazolo[3,4-d]pyrimidine derivatives bearing 5,6-diphenyl-1,2,4-triazine moiety as potential antimicrobial agents. |
| AID334236 | Antimicrobial activity against Epidermophyton floccosum after 10 days by microdilution technique | 2002 | Journal of natural products, Apr, Volume: 65, Issue:4 | Antimicrobial activities of a new schizozygane indoline alkaloid from Schizozygia coffaeoides and the revised structure of isoschizogaline. |
| AID619215 | Antifungal activity against 10'5 CFU/mL Aspergillus clavatus MTCC 1323 after 48 hrs by agar streak dilution method | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Synthesis and studies of novel 2-(4-cyano-3-trifluoromethylphenyl amino)-4-(quinoline-4-yloxy)-6-(piperazinyl/piperidinyl)-s-triazines as potential antimicrobial, antimycobacterial and anticancer agents. |
| AID723703 | Fungicidal activity against Aspergillus flavus ATCC 9643 after 72 hrs by serial subcultivation method | 2013 | Bioorganic & medicinal chemistry, Jan-15, Volume: 21, Issue:2 | Synthesis and biological evaluation of some 5-arylidene-2-(1,3-thiazol-2-ylimino)-1,3-thiazolidin-4-ones as dual anti-inflammatory/antimicrobial agents. |
| AID1429860 | n-octanol-phosphate buffer distribution coefficient, log D of the compound at pH 5.5 after 90 mins by shake-flask method | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Crystal structures, binding interactions, and ADME evaluation of brain penetrant N-substituted indazole-5-carboxamides as subnanomolar, selective monoamine oxidase B and dual MAO-A/B inhibitors. |
| AID551100 | Antifungal activity against Aspergillus flavus by liquid dilution method | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1 | 3-[Benzimidazo- and 3-[benzothiadiazoleimidazo-(1,2-c)quinazolin-5-yl]-2H-chromene-2-ones as potent antimicrobial agents. |
| AID336893 | Antifungal activity against Trichophyton rubrum after 2 to 4 days | |||
| AID681120 | TP_TRANSPORTER: inhibition of Rhodamine 123 efflux in Caco-2 cells | 2003 | Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9 | Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery. |
| AID723700 | Fungicidal activity against Aspergillus niger ATCC 6275 after 72 hrs by serial subcultivation method | 2013 | Bioorganic & medicinal chemistry, Jan-15, Volume: 21, Issue:2 | Synthesis and biological evaluation of some 5-arylidene-2-(1,3-thiazol-2-ylimino)-1,3-thiazolidin-4-ones as dual anti-inflammatory/antimicrobial agents. |
| AID395652 | Antifungal activity against Cryptococcus neoformans ATCC 32264 assessed as growth inhibition at 100 uM after 48 hrs | 2009 | European journal of medicinal chemistry, Jan, Volume: 44, Issue:1 | Penetratin and derivatives acting as antifungal agents. |
| AID49133 | Tested for minimum subinhibitory concentration against Candida albicans 26 (Candida albicans) at pH 6.5. | 1994 | Journal of medicinal chemistry, Jun-24, Volume: 37, Issue:13 | Derivatives of a novel cyclopeptolide. 1. Synthesis, antifungal activity, and structure-activity relationships. |
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| AID417965 | Antimicrobial activity against Aspergillus niger after 48 hrs by broth microdilution technique | 2009 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6 | Relation between lipophilicity of alkyl gallates and antifungal activity against yeasts and filamentous fungi. |
| AID454776 | Antifungal activity against Cryptococcus neoformans ATCC 32264 after 48 hrs by broth microdilution technique | 2009 | Bioorganic & medicinal chemistry, Nov-01, Volume: 17, Issue:21 | 5-Nitrofuranes and 5-nitrothiophenes with anti-Trypanosoma cruzi activity and ability to accumulate squalene. |
| AID447226 | Antifungal activity against Rhodotorula rubra DSM 70403 at 20 ug after 72 hrs by agar disk diffusion assay | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11 | Synthesis, Raman, FT-IR, NMR spectroscopic characterization, antimicrobial activity, cytotoxicity and DNA binding of new mixed aza-oxo-thia macrocyclic compounds. |
| AID1464256 | Inhibition of human CYP27B1 expressed in Escherichia coli assessed as reduction in hydrolase activity incubated for 25 mins using Adx, AdR and 1,25(OH)2D3 | 2017 | Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20 | Analysis of the binding sites of vitamin D 1α-hydroxylase (CYP27B1) and vitamin D 24-hydroxylase (CYP24A1) for the design of selective CYP24A1 inhibitors: Homology modelling, molecular dynamics simulations and identification of key binding requirements. |
| AID386885 | Antibacterial activity against Staphylococcus aureus ATCC 19433 by cup plate method | 2008 | European journal of medicinal chemistry, Oct, Volume: 43, Issue:10 | Condensed bridgehead nitrogen heterocyclic system: synthesis and pharmacological activities of 1,2,4-triazolo-[3,4-b]-1,3,4-thiadiazole derivatives of ibuprofen and biphenyl-4-yloxy acetic acid. |
| AID633964 | Antifungal activity against Trichoderma viride IAM 5061 incubated for 72 hrs followed by serial sub-cultivation for 72 hrs by serial dilution technique | 2011 | Bioorganic & medicinal chemistry, Dec-15, Volume: 19, Issue:24 | Novel (E)-1-(4-methyl-2-(alkylamino)thiazol-5-yl)-3-arylprop-2-en-1-ones as potent antimicrobial agents. |
| AID340954 | Antifungal activity against Candida glabrata ATCC 90030 by NCCLS M27-A2 method | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8 | Cross-resistance to medical and agricultural azole drugs in yeasts from the oropharynx of human immunodeficiency virus patients and from environmental Bavarian vine grapes. |
| AID574255 | Antifungal activity against 48 hrs cultures of 10'7 cells/ml wild-type Candida albicans BF-1 biofilms by XTT reduction assay | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | Cell density and cell aging as factors modulating antifungal resistance of Candida albicans biofilms. |
| AID1263195 | Cytotoxicity against human SKLU1 cells as growth inhibition at 50 uM | 2015 | Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24 | Synthesis and activity of novel 16-dehydropregnenolone acetate derivatives as inhibitors of type 1 5α-reductase and on cancer cell line SK-LU-1. |
| AID322160 | Antifungal activity against Candida parapsilosis C 124-2000 after 48 hrs by CLSI M27-A2 method | 2008 | Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1 | N-Phenyl and N-phenylalkyl-maleimides acting against Candida spp.: time-to-kill, stability, interaction with maleamic acids. |
| AID54923 | Inhibition of human cytochrome P450 3A4 | 2003 | Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9 | Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery. |
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| AID1079944 | Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source] | |||
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| AID294855 | Antifungal activity against Microsporum gypseum after 7 days by micro-broth dilution method | 2007 | European journal of medicinal chemistry, Sep, Volume: 42, Issue:9 | Synthesis of novel triazole derivatives as inhibitors of cytochrome P450 14alpha-demethylase (CYP51). |
| AID204479 | Minimum inhibitory concentration against Sporothrix schenckii | 2004 | Bioorganic & medicinal chemistry letters, Jan-19, Volume: 14, Issue:2 | Synthesis of galactopyranosyl amino alcohols as a new class of antitubercular and antifungal agents. |
| AID319750 | Antimicrobial activity against Candida albicans ATCC 76615 | 2008 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 18, Issue:11 | Synthesis and SAR studies of biaryloxy-substituted triazoles as antifungal agents. |
| AID1472625 | In vitro antifungal activity against Trichophyton verrucosum after 7 days by serial dilution method | 2018 | Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1 | Novel Terminal Bipheny-Based Diapophytoene Desaturases (CrtN) Inhibitors as Anti-MRSA/VISR/LRSA Agents with Reduced hERG Activity. |
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| AID282367 | Inhibition of ATRA-induced CYP26 in human MCF7 cells assessed ATRA as metabolism using [11.12-3H]-ATRA | 2004 | Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27 | Novel retinoic acid metabolism blocking agents endowed with multiple biological activities are efficient growth inhibitors of human breast and prostate cancer cells in vitro and a human breast tumor xenograft in nude mice. |
| AID1168630 | Antimicrobial activity against Candida tropicalis ATCC 13803 at 50 ug after 18 hrs by agar well diffusion assay | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | Phosphorus-nitrogen compounds. Part 29. Syntheses, crystal structures, spectroscopic and stereogenic properties, electrochemical investigations, antituberculosis, antimicrobial and cytotoxic activities and DNA interactions of ansa-spiro-ansa cyclotetrapho |
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| AID53236 | Inhibition of human testicular microsomal Cytochrome P450 17A1 | 1997 | Journal of medicinal chemistry, Sep-26, Volume: 40, Issue:20 | 17-Imidazolyl, pyrazolyl, and isoxazolyl androstene derivatives. Novel steroidal inhibitors of human cytochrome C17,20-lyase (P450(17 alpha). |
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| AID1238339 | Inhibition of CYP3A4 (unknown origin) at 20 uM by luminescent readout-based method | 2015 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 25, Issue:16 | Phenoxymethyl 1,3-oxazoles and 1,2,4-oxadiazoles as potent and selective agonists of free fatty acid receptor 1 (GPR40). |
| AID1166503 | Inhibition of rat liver 5alpha-reductase type 1 assessed as conversion of [3H]testosterone to dihydrotestosterone | 2014 | Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21 | Effect of dehydroepiandrosterone derivatives on the activity of 5α-reductase isoenzymes and on cancer cell line PC-3. |
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| AID1176160 | Inhibition of human recombinant MDR1 in cell membrane fraction preincubated for 5 mins at 1 uM measured after 40 mins by Pgp-Glo luciferase assay | 2015 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2 | Investigating the binding interactions of the anti-Alzheimer's drug donepezil with CYP3A4 and P-glycoprotein. |
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| AID681131 | TP_TRANSPORTER: inhibition of Daunorubicin efflux in NIH-3T3-G185 cells | 2001 | Biochemical and biophysical research communications, Nov-30, Volume: 289, Issue:2 | Active transport of fluorescent P-glycoprotein substrates: evaluation as markers and interaction with inhibitors. |
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| AID575112 | Antifungal activity against Madurella mycetomatis isolate 49 by XTT assay | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Madurella mycetomatis is not susceptible to the echinocandin class of antifungal agents. |
| AID1312607 | Antifungal activity against naftifine-sensitive Trichophyton rubrum after 7 days by serial dilution method | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10 | Discovery of Benzocycloalkane Derivatives Efficiently Blocking Bacterial Virulence for the Treatment of Methicillin-Resistant S. aureus (MRSA) Infections by Targeting Diapophytoene Desaturase (CrtN). |
| AID1171976 | Antibacterial activity against Klebsiella pneumoniae MTCC 109 assessed as zone of inhibition at 1 mg/disc after 24 hrs by disc diffusion method | 2015 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2 | Facile and diastereoselective synthesis of 3,2'-spiropyrrolidine-oxindoles derivatives, their molecular docking and antiproliferative activities. |
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| AID762384 | Antifungal activity against Aspergillus niger ATCC 16404 after 24 to 72 hrs by microdilution method | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | Synthesis, in vitro antifungal activity and in silico study of 3-(1,2,4-triazol-1-yl)flavanones. |
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| AID1171992 | Antibacterial activity against Staphylococcus epidermidis MTCC 3615 assessed as inhibition of visual growth after 24 hrs | 2015 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2 | Facile and diastereoselective synthesis of 3,2'-spiropyrrolidine-oxindoles derivatives, their molecular docking and antiproliferative activities. |
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| AID1474082 | Drug concentration at steady state in human at 200 mg, po QD after 24 hrs | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1 | A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
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| AID463409 | Antimicrobial activity against Candida albicans at 1000 ug after 72 hrs by cup plate method | 2010 | European journal of medicinal chemistry, Mar, Volume: 45, Issue:3 | Antimicrobial study of newly synthesized 6-substituted indolo[1,2-c]quinazolines. |
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| AID323058 | Antifungal activity against Candida tropicalis C131 by micro-broth dilution method | 2008 | Bioorganic & medicinal chemistry, Jan-15, Volume: 16, Issue:2 | Antifungal and cytotoxic activities of some N-substituted aniline derivatives bearing a hetaryl fragment. |
| AID362237 | Inhibition of hepatic CYP2B6 expressed in insect microsomes at 1 uM | 2008 | Bioorganic & medicinal chemistry, Aug-15, Volume: 16, Issue:16 | Synthesis, biological evaluation, and molecular modeling studies of methylene imidazole substituted biaryls as inhibitors of human 17alpha-hydroxylase-17,20-lyase (CYP17)--part II: Core rigidification and influence of substituents at the methylene bridge. |
| AID100099 | Percent decrease in luteinizing hormone concentration, when 100 mg/kg of compound was given intraduodenally | 1989 | Journal of medicinal chemistry, Sep, Volume: 32, Issue:9 | LH-RH antagonists: design and synthesis of a novel series of peptidomimetics. |
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| AID588216 | FDA HLAED, serum glutamic oxaloacetic transaminase (SGOT) increase | 2004 | Current drug discovery technologies, Dec, Volume: 1, Issue:4 | Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling. |
| AID245919 | Cytotoxicity to reduce chronic myeloid leukemia K 562 cells | 2004 | Journal of medicinal chemistry, Jul-29, Volume: 47, Issue:16 | Imidazole analogues of fluoxetine, a novel class of anti-Candida agents. |
| AID214435 | In vitro antifungal activity against Trichophyton tonsurans ATCC 9085 | 1988 | Journal of medicinal chemistry, Oct, Volume: 31, Issue:10 | Studies on antifungal agents. 23. Novel substituted 3,5-diphenyl-3-(1H-imidazol-1-ylmethyl)- 2-alkylisoxazolidine derivatives. |
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| AID407010 | Antimicrobial activity against fluconazole-resistant Candida albicans FH5 dissociated biofilms at cell density of 10'3 cells/ml after 48 hrs by XTT assay | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | Role for cell density in antifungal drug resistance in Candida albicans biofilms. |
| AID652431 | Selectivity ratio of IC50 for human CYP11B2 to IC50 for human CYP11B1 | 2011 | ACS medicinal chemistry letters, Aug-11, Volume: 2, Issue:8 | Optimization of the First Selective Steroid-11β-hydroxylase (CYP11B1) Inhibitors for the Treatment of Cortisol Dependent Diseases. |
| AID1079949 | Proposed mechanism(s) of liver damage. [column 'MEC' in source] | |||
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| AID619217 | Antifungal activity against 10'5 CFU/mL Candida albicans MTCC 183 after 48 hrs by agar streak dilution method | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Synthesis and studies of novel 2-(4-cyano-3-trifluoromethylphenyl amino)-4-(quinoline-4-yloxy)-6-(piperazinyl/piperidinyl)-s-triazines as potential antimicrobial, antimycobacterial and anticancer agents. |
| AID285161 | Antimicrobial activity against non replicating persistence Mycobacterium tuberculosis H37Rv in anaerobic condition assessed as relative light unit after 11 days by LORA assay | 2007 | Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4 | Low-oxygen-recovery assay for high-throughput screening of compounds against nonreplicating Mycobacterium tuberculosis. |
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| AID632561 | Antibacterial activity against Bacillus pumilus at 200 ug/mL after 24 hrs by agar cup diffusion method | 2011 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 21, Issue:24 | A new antifungal briarane diterpenoid from the gorgonian Junceella juncea Pallas. |
| AID323064 | Antifungal activity against Microsporum gypseum C115 by microbroth dilution method | 2008 | Bioorganic & medicinal chemistry, Jan-15, Volume: 16, Issue:2 | Antifungal and cytotoxic activities of some N-substituted aniline derivatives bearing a hetaryl fragment. |
| AID363774 | Antimicrobial activity against Cryptococcus neoformans ATCC 32264 at 6.25 ug/ml after 48 hrs | 2008 | Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17 | In vitro antifungal activity of polyfunctionalized 2-(hetero)arylquinolines prepared through imino Diels-Alder reactions. |
| AID687502 | Antifungal activity against Cryptococcus neoformans ATCC 32264 after 48 hrs by NCCLS broth microdilution method | 2012 | Bioorganic & medicinal chemistry, Oct-15, Volume: 20, Issue:20 | Structure-activity relationship study of nitrosopyrimidines acting as antifungal agents. |
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| AID395380 | Antifungal activity against Debaryomyces hansenii DSM 70238 at 1 ug after 72 hrs by disk diffusion method | 2009 | European journal of medicinal chemistry, Jan, Volume: 44, Issue:1 | Synthesis, Raman, FT-IR, NMR spectroscopic data and antimicrobial activity of mixed aza-oxo-thia macrocyclic compounds. |
| AID1247084 | Antifungal activity against Candida albicans assessed as growth inhibition at 1 mg/well after 48 hrs by Well method | 2015 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19 | Synthesis of BF₃ catalyzed Mannich derivatives with excellent ee from phenylpropanolamine, study of their antimicrobial activity and molecular docking. |
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| AID555816 | Antifungal activity against azole-resistant Candida albicans 5674 after 48 hrs | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | Relative contributions of the Candida albicans ABC transporters Cdr1p and Cdr2p to clinical azole resistance. |
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| AID419396 | Antifungal activity against Aspergillus niger ATCC 9029 after 48 hrs by agar streak dilution method | 2009 | European journal of medicinal chemistry, May, Volume: 44, Issue:5 | Synthesis and anti-microbial screening of some Schiff bases of 3-amino-6,8-dibromo-2-phenylquinazolin-4(3H)-ones. |
| AID1155879 | Cytotoxicity against mouse J774 cells assessed as growth inhibition at 50 uM after 48 hrs by SRB method | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Synthesis and cytotoxic effect on cancer cell lines and macrophages of novel progesterone derivatives having an ester or a carbamate function at C-3 and C-17. |
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| AID637040 | Antifungal activity against Aspergillus clavatus at 100 ug/disc after 24 hrs by disc diffusion method | 2012 | European journal of medicinal chemistry, Feb, Volume: 48 | Synthesis and biological evaluation of some thiazolidinones as antimicrobial agents. |
| AID1319263 | Inhibition of CYP3A4 in human liver microsomes using midazolam as substrate assessed as reduction in 4-OH-midazolam formation at 0.005 uM by LC/MS/MS analysis | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18 | Identification of (R)-(2-Chloro-3-(trifluoromethyl)phenyl)(1-(5-fluoropyridin-2-yl)-4-methyl-6,7-dihydro-1H-imidazo[4,5-c]pyridin-5(4H)-yl)methanone (JNJ 54166060), a Small Molecule Antagonist of the P2X7 receptor. |
| AID454774 | Antifungal activity against Candida tropicalis C131-2000 after 48 hrs by broth microdilution technique | 2009 | Bioorganic & medicinal chemistry, Nov-01, Volume: 17, Issue:21 | 5-Nitrofuranes and 5-nitrothiophenes with anti-Trypanosoma cruzi activity and ability to accumulate squalene. |
| AID407021 | Antimicrobial activity against Chk1 deficient Candida albicans CHK21 dissociated biofilms at cell density of 10'8 cells/ml after 48 hrs by XTT assay | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | Role for cell density in antifungal drug resistance in Candida albicans biofilms. |
| AID1176157 | Inhibition of human recombinant CYP3A4 expressed in insect cell microsomes preincubated for 10 mins by fluorescence assay | 2015 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2 | Investigating the binding interactions of the anti-Alzheimer's drug donepezil with CYP3A4 and P-glycoprotein. |
| AID632003 | Toxicity in CBA mouse infected with Leishmania amazonensis MHOM/ BR/77/LTB0016 assessed as change in monocytes count at 50 mg/kg, po qd for 30 days administered 4 week post infection measured up to week 21 | 2011 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 21, Issue:24 | Synthesis and antileishmanial evaluation of 1-aryl-4-(4,5-dihydro-1H-imidazol-2-yl)-1H-pyrazole derivatives. |
| AID688635 | Antifungal activity against Aspergillus niger at 100 ug after 48 hrs by agar well diffusion method | 2011 | European journal of medicinal chemistry, Nov, Volume: 46, Issue:11 | Synthesis and antimicrobial activity of amido linked pyrrolyl and pyrazolyl-oxazoles, thiazoles and imidazoles. |
| AID125799 | In vitro antifungal activity against Microsporum audouinii ATCC 9079 | 1988 | Journal of medicinal chemistry, Oct, Volume: 31, Issue:10 | Studies on antifungal agents. 23. Novel substituted 3,5-diphenyl-3-(1H-imidazol-1-ylmethyl)- 2-alkylisoxazolidine derivatives. |
| AID554705 | Antimicrobial activity against Candida krusei B2399 after 48 hrs by liquid microdilution assay | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2 | Abc1p is a multidrug efflux transporter that tips the balance in favor of innate azole resistance in Candida krusei. |
| AID628507 | Antifungal activity against Fusarium solani at 100 ug/ml after 48 hrs by disc diffusion method | 2011 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21 | Synthesis and biological evaluation of some novel triazol-3-ones as antimicrobial agents. |
| AID245190 | Minimum inhibitory concentration to inhibit Candida albicans strain range is equal to 2-16 | 2004 | Journal of medicinal chemistry, Jul-29, Volume: 47, Issue:16 | Imidazole analogues of fluoxetine, a novel class of anti-Candida agents. |
| AID150752 | Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay | 2003 | Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9 | Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery. |
| AID249257 | Antifungal activity to cause 99% reduction of surviving cells in 50% isolates | 2004 | Journal of medicinal chemistry, Jul-29, Volume: 47, Issue:16 | Imidazole analogues of fluoxetine, a novel class of anti-Candida agents. |
| AID687551 | Antifungal activity against Trichophyton mentagrophytes ATCC 9972 by NCCLS broth microdilution method | 2012 | Bioorganic & medicinal chemistry, Oct-15, Volume: 20, Issue:20 | Structure-activity relationship study of nitrosopyrimidines acting as antifungal agents. |
| AID415951 | Antimicrobial activity against Candida parapsilosis by micro-broth dilution method | 2009 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6 | Design, synthesis, and biological evaluation of novel 1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluorophenyl)-3-substituted benzylamino-2-propanols. |
| AID363712 | Antifungal activity against Cryptococcus neoformans ATCC 32264 after 48 hrs by broth microdilution technique | 2008 | Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17 | In vitro antifungal activity of polyfunctionalized 2-(hetero)arylquinolines prepared through imino Diels-Alder reactions. |
| AID515014 | Antifungal activity against Candida kefyr by micro-broth dilution method | 2010 | European journal of medicinal chemistry, Oct, Volume: 45, Issue:10 | Synthesis and antifungal evaluation of novel triazole derivatives as inhibitors of cytochrome P450 14alpha-demethylase. |
| AID363718 | Antifungal activity against Trichophyton mentagrophytes ATCC 9972 after 48 hrs by broth microdilution technique | 2008 | Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17 | In vitro antifungal activity of polyfunctionalized 2-(hetero)arylquinolines prepared through imino Diels-Alder reactions. |
| AID1110736 | Antifungal activity against Aspergillus fumigatus 231 after 48 hr by microdilution broth method | 2002 | Farmaco (Societa chimica italiana : 1989), Feb, Volume: 57, Issue:2 | Ring substituted 3-phenyl-1-(2-pyrazinyl)-2-propen-1-ones as potential photosynthesis-inhibiting, antifungal and antimycobacterial agents. |
| AID125941 | In vitro evaluation of minimum inhibitory concentration against Microsporum canis 47 | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20 | Synthesis and antifungal activity of new azole derivatives containing an N-acylmorpholine ring. |
| AID1210014 | Inhibition of recombinant CYP2J2 (unknown origin)-mediated astemizole O-demethylation assessed as remaining activity at 30 uM after 5 mins by LC-MS/MS analysis relative to control | 2012 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5 | Identifying a selective substrate and inhibitor pair for the evaluation of CYP2J2 activity. |
| AID284340 | Growth inhibition of Candida albicans JRW#5 | 2007 | Bioorganic & medicinal chemistry, Jan-01, Volume: 15, Issue:1 | Design of endoperoxides with anti-Candida activity. |
| AID340016 | Inhibition of refampicin-mediated PXR activation in HepG2 cells | 2008 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14 | Synthesis of novel ketoconazole derivatives as inhibitors of the human Pregnane X Receptor (PXR; NR1I2; also termed SXR, PAR). |
| AID1184069 | Inhibition of IDO1 (unknown origin) using L-tryptophan substrate incubated for 60 mins in presence of 0.01% Triton-X by HPLC | 2014 | European journal of medicinal chemistry, Sep-12, Volume: 84 | Detailed analysis and follow-up studies of a high-throughput screening for indoleamine 2,3-dioxygenase 1 (IDO1) inhibitors. |
| AID405052 | Antifungal activity against Sporothrix schenckii PGAC0016 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by Sensititre YeastOne method | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods. |
| AID307394 | Antifungal activity against Candida glabrata ATCC 34138 by broth microdilution assay | 2007 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12 | Discovery of novel indazole-linked triazoles as antifungal agents. |
| AID313543 | Inhibition of human CYP17 expressed in Escherichia coli | 2008 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 18, Issue:1 | Synthesis, biological evaluation and molecular modelling studies of novel ACD- and ABD-ring steroidomimetics as inhibitors of CYP17. |
| AID696539 | Antifungal activity against Cryptococcus neoformans ATCC 32264 after 48 hrs by broth microdilution technique | 2012 | Bioorganic & medicinal chemistry, Nov-01, Volume: 20, Issue:21 | Synthesis and antifungal activity of diverse C-2 pyridinyl and pyridinylvinyl substituted quinolines. |
| AID420660 | Antifungal activity against Candida albicans ATCC 76615 after 24 hrs by micro-broth dilution method | 2009 | European journal of medicinal chemistry, May, Volume: 44, Issue:5 | Design, synthesis, and biological evaluation of novel triazole derivatives as inhibitors of cytochrome P450 14alpha-demethylase. |
| AID454779 | Antifungal activity against Aspergillus flavus ATCC 9170 after 48 hrs by broth microdilution technique | 2009 | Bioorganic & medicinal chemistry, Nov-01, Volume: 17, Issue:21 | 5-Nitrofuranes and 5-nitrothiophenes with anti-Trypanosoma cruzi activity and ability to accumulate squalene. |
| AID1275147 | Antifungal activity against Candida parapsilosis NRLL Y-12696 after 48 hrs by broth microdilution method | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Synthesis and biological evaluation of new naphthalene substituted thiosemicarbazone derivatives as potent antifungal and anticancer agents. |
| AID456690 | Antifungal activity against Candida albicans ATCC 10231 assessed as inhibition of fungal growth at 50 uM after 24 hrs by microbroth dilution method | 2010 | Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1 | New small-size peptides possessing antifungal activity. |
| AID205796 | Fungicidal concentration on sterol 14-alpha-demethylase | 2003 | Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21 | Identification and prediction of promiscuous aggregating inhibitors among known drugs. |
| AID330532 | Antifungal activity against Candida parapsilosis infected cyclophosphamide-immunocompromized Crl:CD1(ICR) mouse assessed as fungal density in lung at 50 mg/kg, po for 5 days measured on day 12 | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Mar-13, Volume: 104, Issue:11 | High-throughput synergy screening identifies microbial metabolites as combination agents for the treatment of fungal infections. |
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| AID600777 | Fungicidal activity against Trichoderma viride IAM 5061 after 72 hrs | 2011 | Bioorganic & medicinal chemistry, May-15, Volume: 19, Issue:10 | Thiazole-based chalcones as potent antimicrobial agents. Synthesis and biological evaluation. |
| AID1184070 | Inhibition of mouse IDO1 expressed in mouse P815B cells using L-tryptophan substrate incubated for 18 hrs by HPLC based cellular assay | 2014 | European journal of medicinal chemistry, Sep-12, Volume: 84 | Detailed analysis and follow-up studies of a high-throughput screening for indoleamine 2,3-dioxygenase 1 (IDO1) inhibitors. |
| AID402394 | Antifungal activity against Saccharomyces cerevisiae 1138 | 1998 | Journal of natural products, Oct, Volume: 61, Issue:10 | DNA-damaging steroidal alkaloids from Eclipta alba from the suriname rainforest1. |
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| AID1171990 | Antibacterial activity against Micrococcus luteus MTCC 106 assessed as inhibition of visual growth after 24 hrs | 2015 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2 | Facile and diastereoselective synthesis of 3,2'-spiropyrrolidine-oxindoles derivatives, their molecular docking and antiproliferative activities. |
| AID405061 | Antifungal activity against Sporothrix schenckii P30915 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by Sensititre YeastOne method | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods. |
| AID362164 | Inhibition of human recombinant CYP17 expressed in Escherichia coli coexpressing NADPH-P450 reductase | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16 | Synthesis, biological evaluation, and molecular modeling of abiraterone analogues: novel CYP17 inhibitors for the treatment of prostate cancer. |
| AID613260 | Antifungal activity against Candida albicans ATCC 10231 after 24 hrs by NCCLS M38-P broth dilution method | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Design, synthesis and antimicrobial activity of chiral 2-(substituted-hydroxyl)-3-(benzo[d]oxazol-5-yl)propanoic acid derivatives. |
| AID699541 | Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake at 20 uM incubated for 5 mins by scintillation counting | 2012 | Journal of medicinal chemistry, May-24, Volume: 55, Issue:10 | Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions. |
| AID315663 | Inhibition of recombinant CYP2B6 at 1 uM | 2008 | Bioorganic & medicinal chemistry, Feb-15, Volume: 16, Issue:4 | Synthesis, biological evaluation and molecular modelling studies of methyleneimidazole substituted biaryls as inhibitors of human 17alpha-hydroxylase-17,20-lyase (CYP17). Part I: Heterocyclic modifications of the core structure. |
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| AID83862 | Effect on total serum cholesterol in male hamsters at a dose of 25 mg/kg orally administered for 14 days | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | Selective inhibition of mammalian lanosterol 14 alpha-demethylase: a possible strategy for cholesterol lowering. |
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| AID376044 | Antifungal activity against Epidermophyton floccosum C 114 up to 50 ug/mL by agar dilution method | 1999 | Journal of natural products, Oct, Volume: 62, Issue:10 | In vitro evaluation of antifungal properties of phenylpropanoids and related compounds acting against dermatophytes. |
| AID100101 | Dissociation constant was determined in vitro using rat pituitary membranes and [125I]leuprolide as radioligand, at concentration 3.16*10e-5 M | 1989 | Journal of medicinal chemistry, Sep, Volume: 32, Issue:9 | LH-RH antagonists: design and synthesis of a novel series of peptidomimetics. |
| AID689078 | Antimicrobial activity against Chlorella fusca assessed as zone of inhibition at 0.05 mg by agar diffusion method | 2012 | Journal of natural products, Sep-28, Volume: 75, Issue:9 | Sinularosides A and B, bioactive 9,11-secosteroidal glycosides from the South China Sea soft coral Sinularia humilis Ofwegen. |
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| AID1557086 | Antifungal activity against Candida albicans SN152 assessed as reduction in fungal cell growth incubated for 48 hrs by MTT based broth double dilution method | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Antifungal activity, mode of action variability, and subcellular distribution of coumarin-based antifungal azoles. |
| AID599148 | Antibacterial activity against Pseudomonas fluorescens after 24 hrs by MTT assay | 2008 | European journal of medicinal chemistry, Mar, Volume: 43, Issue:3 | Synthesis, crystal structure and antimicrobial activity of deoxybenzoin derivatives from genistein. |
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| AID91481 | Binding constant against human serum albumin (HSA) | 2001 | Journal of medicinal chemistry, Dec-06, Volume: 44, Issue:25 | Cheminformatic models to predict binding affinities to human serum albumin. |
| AID49096 | The compound was tested for antifungal activity against Candida albicans My1029 using agar dilution assay | 1987 | Journal of medicinal chemistry, Aug, Volume: 30, Issue:8 | Lysosomotropic agents. 7. Broad-spectrum antifungal activity of lysosomotropic detergents. |
| AID1328450 | Inhibition of recombinant CYP11B1 (unknown origin) overexpressed in human AD293 cells assessed as reduction in cortisol formation preincubated for 60 mins followed by addition of 11-deoxycortisol as substrate measured after 12 hrs by LC-MS/MS analysis | 2016 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 26, Issue:23 | Design, synthesis, and evaluation of (2S,4R)-Ketoconazole sulfonamide analogs as potential treatments for Metabolic Syndrome. |
| AID624626 | Ratio of apparent permeability from basolateral to apical side over apical to basolateral side determined in MDR1-MDCKII cells | 2001 | The Journal of pharmacology and experimental therapeutics, Nov, Volume: 299, Issue:2 | Rational use of in vitro P-glycoprotein assays in drug discovery. |
| AID376054 | Antifungal activity against Aspergillus niger ATCC 9029 by agar dilution method | 1999 | Journal of natural products, Oct, Volume: 62, Issue:10 | In vitro evaluation of antifungal properties of phenylpropanoids and related compounds acting against dermatophytes. |
| AID633963 | Antifungal activity against Penicillium ochrochloron ATCC 9112 incubated for 72 hrs followed by serial sub-cultivation for 72 hrs by serial dilution technique | 2011 | Bioorganic & medicinal chemistry, Dec-15, Volume: 19, Issue:24 | Novel (E)-1-(4-methyl-2-(alkylamino)thiazol-5-yl)-3-arylprop-2-en-1-ones as potent antimicrobial agents. |
| AID1155877 | Cytotoxicity against human MCF7 cells assessed as growth inhibition at 50 uM after 48 hrs by SRB method | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Synthesis and cytotoxic effect on cancer cell lines and macrophages of novel progesterone derivatives having an ester or a carbamate function at C-3 and C-17. |
| AID486241 | Antifungal activity against Microsporum gypseum C 115 after 48 hrs | 2010 | European journal of medicinal chemistry, Jun, Volume: 45, Issue:6 | Naftifine-analogues as anti-Trypanosoma cruzi agents. |
| AID50305 | The compound was tested for antifungal activity against Candida krusei MY1020 using agar dilution assay | 1987 | Journal of medicinal chemistry, Aug, Volume: 30, Issue:8 | Lysosomotropic agents. 7. Broad-spectrum antifungal activity of lysosomotropic detergents. |
| AID214293 | Inhibition of Trichophyton mentagrophytes 445 growth for 72 hours in vitro. | 2001 | Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17 | 3-Phenyl-5-acyloxymethyl-2H,5H-furan-2-ones: synthesis and biological activity of a novel group of potential antifungal drugs. |
| AID1304741 | Antifungal activity against Microsporum gypseum measured after 7 days by serial dilution method | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7 | Discovery of Potent Benzofuran-Derived Diapophytoene Desaturase (CrtN) Inhibitors with Enhanced Oral Bioavailability for the Treatment of Methicillin-Resistant Staphylococcus aureus (MRSA) Infections. |
| AID575109 | Antifungal activity against Madurella mycetomatis isolate 43 by XTT assay | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Madurella mycetomatis is not susceptible to the echinocandin class of antifungal agents. |
| AID681139 | TP_TRANSPORTER: increase in dihydrofluorescein intracellular accumulation (dihydrofluorescein: 1 uM) in SK-E2 cells (expressing BSEP) | 2003 | Pharmaceutical research, Apr, Volume: 20, Issue:4 | Fluorescent substrates of sister-P-glycoprotein (BSEP) evaluated as markers of active transport and inhibition: evidence for contingent unequal binding sites. |
| AID481673 | Cytotoxicity against african pig LLC-PK11 up to 25 ug/ml after 48 hrs by neutral red assay | 2010 | European journal of medicinal chemistry, May, Volume: 45, Issue:5 | Synthesis and the selective antifungal activity of 5,6,7,8-tetrahydroimidazo[1,2-a]pyridine derivatives. |
| AID315666 | Inhibition of recombinant CYP2D6 at 10 uM | 2008 | Bioorganic & medicinal chemistry, Feb-15, Volume: 16, Issue:4 | Synthesis, biological evaluation and molecular modelling studies of methyleneimidazole substituted biaryls as inhibitors of human 17alpha-hydroxylase-17,20-lyase (CYP17). Part I: Heterocyclic modifications of the core structure. |
| AID554724 | Fold resistant, ratio of MIC for Saccharomyces cerevisiae isolate ADdelta overexpressing Candida krusei ERG11C to MIC for Saccharomyces cerevisiae isolate ADdelta overexpressing Abc1p | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2 | Abc1p is a multidrug efflux transporter that tips the balance in favor of innate azole resistance in Candida krusei. |
| AID636990 | Antifungal activity against Aspergillus niger after 48 hrs by agar streak dilution method | 2012 | European journal of medicinal chemistry, Feb, Volume: 48 | Synthesis and biological evaluation of some thiazolidinones as antimicrobial agents. |
| AID1196738 | Antifungal activity against Candida parapsilosis NRLL Y 12696 after 48 hrs by broth microdilution assay | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | A novel series of thiazolyl-pyrazoline derivatives: synthesis and evaluation of antifungal activity, cytotoxicity and genotoxicity. |
| AID555330 | Antimicrobial activity against Candida krusei ATCC 6258 by EUCAST broth microdilution method | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Fenticonazole activity measured by the methods of the European Committee on Antimicrobial Susceptibility Testing and CLSI against 260 Candida vulvovaginitis isolates from two European regions and annotations on the prevalent genotypes. |
| AID1129509 | Antimicrobial activity against Aspergillus niger at 100 ug/well after 48 hrs by agar well diffusion method | 2014 | European journal of medicinal chemistry, Apr-22, Volume: 77 | Synthesis, antimicrobial and cytotoxic activities of pyrimidinyl benzoxazole, benzothiazole and benzimidazole. |
| AID395378 | Antifungal activity against Rhodotorula rubra DSM 70403 at 1 ug after 72 hrs by disk diffusion method | 2009 | European journal of medicinal chemistry, Jan, Volume: 44, Issue:1 | Synthesis, Raman, FT-IR, NMR spectroscopic data and antimicrobial activity of mixed aza-oxo-thia macrocyclic compounds. |
| AID287721 | Inhibition of human recombinant aromatase at 1 uM after 30 mins relative to control | 2007 | Bioorganic & medicinal chemistry, Apr-01, Volume: 15, Issue:7 | Synthesis of DL-standishinal and its related compounds for the studies on structure-activity relationship of inhibitory activity against aromatase. |
| AID55189 | The compound was tested for antifungal activity against Cryptococcus neoformans MY1146 using agar dilution assay | 1987 | Journal of medicinal chemistry, Aug, Volume: 30, Issue:8 | Lysosomotropic agents. 7. Broad-spectrum antifungal activity of lysosomotropic detergents. |
| AID532571 | Antifungal activity against Candida glabrata isolate 21230 with silent mutations in ERG4, ERG5 genes and nonsense mutation in ERG6 gene by disk diffusion method | 2008 | Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10 | A nonsense mutation in the ERG6 gene leads to reduced susceptibility to polyenes in a clinical isolate of Candida glabrata. |
| AID655585 | Antifungal activity against Candida kefyr by microbroth dilution method | 2012 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8 | New triazole derivatives as antifungal agents: synthesis via click reaction, in vitro evaluation and molecular docking studies. |
| AID396961 | Antifungal activity against Curvularia lunata NCIM 716 at 200 ug/disk after 48 hrs by agar disc-diffusion method | 2009 | European journal of medicinal chemistry, May, Volume: 44, Issue:5 | Synthesis, antimicrobial and cytotoxic activities of 1,3,4-oxadiazoles, 1,3,4-thiadiazoles and 1,2,4-triazoles. |
| AID574258 | Antifungal activity against 24 hrs cultures of 10'7 cells/ml Candida albicans SC5314 biofilms by XTT reduction assay | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | Cell density and cell aging as factors modulating antifungal resistance of Candida albicans biofilms. |
| AID1310917 | Inhibition of recombinant human CYP3A4 by P450-Glo luminescence assay | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10 | 2-(3-Methoxyphenyl)quinazoline Derivatives: A New Class of Direct Constitutive Androstane Receptor (CAR) Agonists. |
| AID499539 | Inhibition of human CYP17 expressed in Escherichia coli | 2010 | Journal of medicinal chemistry, Aug-12, Volume: 53, Issue:15 | Replacement of imidazolyl by pyridyl in biphenylmethylenes results in selective CYP17 and dual CYP17/CYP11B1 inhibitors for the treatment of prostate cancer. |
| AID362812 | Antifungal activity against Aspergillus niger at 100 ug after 48 hrs by agar disc-diffusion method | 2008 | European journal of medicinal chemistry, May, Volume: 43, Issue:5 | Synthesis and antimicrobial activity of novel sulfone-linked bis heterocycles. |
| AID348155 | Cytotoxicity against mouse J774 cells after 48 hrs by MTT assay | 2009 | Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2 | Synthesis, trypanocidal activity and docking studies of novel quinoxaline-N-acylhydrazones, designed as cruzain inhibitors candidates. |
| AID616869 | Antimicrobial activity against Aerobacter aerogenes after 24 hrs by agar dilution method | 2011 | Journal of natural products, Aug-26, Volume: 74, Issue:8 | Cytotoxic bipyridines from the marine-derived actinomycete Actinoalloteichus cyanogriseus WH1-2216-6. |
| AID1130398 | Antifungal activity against Candida albicans B2630 infected in guinea pig cutaneous candidosis model at 0.63 mg/kg, po for 14 days measured on day 21 | 1979 | Journal of medicinal chemistry, Aug, Volume: 22, Issue:8 | Antimycotic imidazoles. part 4. Synthesis and antifungal activity of ketoconazole, a new potent orally active broad-spectrum antifungal agent. |
| AID1195126 | Inhibition of human recombinant CYP3A4 assessed as effect on conversion of beetle D-luciferin derivative into D-luciferin by firefly luciferase based luminescence assay | 2015 | Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10 | Design, synthesis and biological evaluation of new hybrid anticonvulsants derived from N-benzyl-2-(2,5-dioxopyrrolidin-1-yl)propanamide and 2-(2,5-dioxopyrrolidin-1-yl)butanamide derivatives. |
| AID429372 | Antifungal activity against Candida albicans after 72 hrs by liquid dilution method | 2009 | European journal of medicinal chemistry, Aug, Volume: 44, Issue:8 | Mono and bis-6-arylbenzimidazo[1,2-c]quinazolines: a new class of antimicrobial agents. |
| AID48431 | Tested In vitro for antifungal activity against candida Spp (Candida glabrata, Candida krusei) at pH 5.8 | 2002 | Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13 | Antifungal agents. 10. New derivatives of 1-[(aryl)[4-aryl-1H-pyrrol-3-yl]methyl]-1H-imidazole, synthesis, anti-candida activity, and quantitative structure-analysis relationship studies. |
| AID330521 | Antifungal activity against Candida parapsilosis infected cyclophosphamide-immunocompromized Crl:CD1(ICR) mouse assessed as survival at 0.5 mg/kg, po for 5 days | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Mar-13, Volume: 104, Issue:11 | High-throughput synergy screening identifies microbial metabolites as combination agents for the treatment of fungal infections. |
| AID1496822 | Inhibition of CYP3A4 in human liver microsomes assessed as testosterone 6beta-hydroxylation after 4 to 40 mins in presence of NADPH by LCMS analysis | 2018 | Bioorganic & medicinal chemistry, 07-15, Volume: 26, Issue:11 | Synthesis and profiling of benzylmorpholine 1,2,4,5-tetraoxane analogue N205: Towards tetraoxane scaffolds with potential for single dose cure of malaria. |
| AID1165071 | Inhibition of N-terminally MBP-fused human CYP24A1 by cell-free assay | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | Novel styryl-indoles as small molecule inhibitors of 25-hydroxyvitamin D-24-hydroxylase (CYP24A1): Synthesis and biological evaluation. |
| AID330531 | Antifungal activity against Candida parapsilosis infected cyclophosphamide-immunocompromized Crl:CD1(ICR) mouse assessed as fungal density in lung at 10 mg/kg, po for 5 days measured on day 12 | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Mar-13, Volume: 104, Issue:11 | High-throughput synergy screening identifies microbial metabolites as combination agents for the treatment of fungal infections. |
| AID48051 | Minimum inhibitory concentration of compound for antifungal activity against Candida parapsilosis | 2000 | Bioorganic & medicinal chemistry letters, Oct-02, Volume: 10, Issue:19 | Novel antifungals based on 4-substituted imidazole: a combinatorial chemistry approach to lead discovery and optimization. |
| AID1057769 | Antimicrobial activity against Candida krusei ATCC 6258 after 24 hrs by broth microdilution method | 2013 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24 | Synthesis and initial biological evaluation of substituted 1-phenylamino-2-thio-4,5-dimethyl-1H-imidazole derivatives. |
| AID1557075 | Antifungal activity against Candida albicans ATCC 90028 assessed as reduction in fungal cell growth incubated for 24 hrs by MTT based broth double dilution method | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Antifungal activity, mode of action variability, and subcellular distribution of coumarin-based antifungal azoles. |
| AID405043 | Antifungal activity against Sporothrix schenckii P1621 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by Sensititre YeastOne method | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods. |
| AID208343 | Enhanced styrene oxide hydrolase activity pH 8.7 | 1985 | Journal of medicinal chemistry, Aug, Volume: 28, Issue:8 | Structural features of imidazole derivatives that enhance styrene oxide hydrolase activity in rat hepatic microsomes. |
| AID532530 | Antifungal activity against Saccharomyces cerevisiae BY4741 harboring human CYP51 assessed as accumulation of 14-alpha-methylergosta-8,24(28)-dien-3beta-6alpha-diol at 4 ug/ml | 2008 | Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10 | Differential azole antifungal efficacies contrasted using a Saccharomyces cerevisiae strain humanized for sterol 14 alpha-demethylase at the homologous locus. |
| AID402399 | Cytotoxicity against mouse M109 cells | 1998 | Journal of natural products, Oct, Volume: 61, Issue:10 | DNA-damaging steroidal alkaloids from Eclipta alba from the suriname rainforest1. |
| AID600771 | Antifungal activity against Penicillium funiculosum ATCC 36839 after 72 hrs by serial dilution method | 2011 | Bioorganic & medicinal chemistry, May-15, Volume: 19, Issue:10 | Thiazole-based chalcones as potent antimicrobial agents. Synthesis and biological evaluation. |
| AID343556 | Antitrypanosomal activity against epimastigotes of Trypanosoma cruzi Tulahuen 2 at 25 uM relative to control | 2008 | Bioorganic & medicinal chemistry, Jul-15, Volume: 16, Issue:14 | New trypanocidal hybrid compounds from the association of hydrazone moieties and benzofuroxan heterocycle. |
| AID454772 | Selectivity index, ratio of IC50 for mouse J774 cells to ID50 for Trypanosoma cruzi tulahuen 2 | 2009 | Bioorganic & medicinal chemistry, Nov-01, Volume: 17, Issue:21 | 5-Nitrofuranes and 5-nitrothiophenes with anti-Trypanosoma cruzi activity and ability to accumulate squalene. |
| AID532565 | Antifungal activity against wild-type Saccharomyces cerevisiae BY4741 by broth microdilution method | 2008 | Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10 | Differential azole antifungal efficacies contrasted using a Saccharomyces cerevisiae strain humanized for sterol 14 alpha-demethylase at the homologous locus. |
| AID1166506 | Cytotoxicity against human PC3 cells assessed as growth inhibition at 50 uM after 48 hrs by SRB assay | 2014 | Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21 | Effect of dehydroepiandrosterone derivatives on the activity of 5α-reductase isoenzymes and on cancer cell line PC-3. |
| AID282369 | Inhibition of ATRA-induced CYP26 in human T47D cell microsome assessed as ATRA metabolism using [11.12-3H]-ATRA | 2004 | Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27 | Novel retinoic acid metabolism blocking agents endowed with multiple biological activities are efficient growth inhibitors of human breast and prostate cancer cells in vitro and a human breast tumor xenograft in nude mice. |
| AID533802 | Antifungal activity against Microsporum gypseum C115 by agar dilution method | 2010 | European journal of medicinal chemistry, Nov, Volume: 45, Issue:11 | Synthesis and biological evaluation of N-antipyrine-4-substituted amino-3-chloromaleimide derivatives. |
| AID449687 | Antifungal activity against Curvularia lunata NCIM 716 at 200 ug/disk after 48 hrs by agar disk diffusion method | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11 | Synthesis, antimicrobial and antioxidant activities of substituted pyrazoles, isoxazoles, pyrimidine and thioxopyrimidine derivatives. |
| AID765650 | Antifungal activity against Candida albicans NRRLY 477 assessed as growth inhibition at 0.5 mg/mL after 24 hrs by agar well diffusion assay | 2013 | European journal of medicinal chemistry, Sep, Volume: 67 | Synthesis of thiosemicarbazones derived from N-(4-hippuric acid)thiosemicarbazide and different carbonyl compounds as antimicrobial agents. |
| AID355423 | Antifungal activity against Candida albicans ATCC 3153 after 18 hrs by broth microdilution method | 2003 | Journal of natural products, Dec, Volume: 66, Issue:12 | New triterpene glycosides from the stems of Anomospermum grandifolium. |
| AID407011 | Antimicrobial activity against fluconazole-resistant Candida albicans FH5 dissociated biofilms at cell density of 10'8 cells/ml after 48 hrs by XTT assay | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | Role for cell density in antifungal drug resistance in Candida albicans biofilms. |
| AID1319265 | Inhibition of CYP3A4 in human liver microsomes using midazolam as substrate assessed as reduction in 4-OH-midazolam formation at 0.02 uM by LC/MS/MS analysis | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18 | Identification of (R)-(2-Chloro-3-(trifluoromethyl)phenyl)(1-(5-fluoropyridin-2-yl)-4-methyl-6,7-dihydro-1H-imidazo[4,5-c]pyridin-5(4H)-yl)methanone (JNJ 54166060), a Small Molecule Antagonist of the P2X7 receptor. |
| AID396962 | Antifungal activity against Aspergillus niger NCIM 596 at 200 ug/disk after 48 hrs by agar disc-diffusion method | 2009 | European journal of medicinal chemistry, May, Volume: 44, Issue:5 | Synthesis, antimicrobial and cytotoxic activities of 1,3,4-oxadiazoles, 1,3,4-thiadiazoles and 1,2,4-triazoles. |
| AID303383 | Selectivity index, ratio of IC50 for human THP1 cells to IC50 for Trypanosoma cruzi CL Brener | 2007 | Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24 | In vivo anti-Chagas vinylthio-, vinylsulfinyl-, and vinylsulfonylbenzofuroxan derivatives. |
| AID386886 | Antibacterial activity against sEscherichia coli ATCC 25922 by cup plate method | 2008 | European journal of medicinal chemistry, Oct, Volume: 43, Issue:10 | Condensed bridgehead nitrogen heterocyclic system: synthesis and pharmacological activities of 1,2,4-triazolo-[3,4-b]-1,3,4-thiadiazole derivatives of ibuprofen and biphenyl-4-yloxy acetic acid. |
| AID600773 | Fungicidal activity against Aspergillus ochraceus ATCC 12066 after 72 hrs | 2011 | Bioorganic & medicinal chemistry, May-15, Volume: 19, Issue:10 | Thiazole-based chalcones as potent antimicrobial agents. Synthesis and biological evaluation. |
| AID45328 | Evaluation of In vitro antifungal activity against Candida albicans ATCC 10231 by broth macro dilution method | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20 | Synthesis and antifungal activity of new azole derivatives containing an N-acylmorpholine ring. |
| AID1061741 | Antimicrobial activity against Candida parapsilosis by broth microdilution method | 2014 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1 | Synthesis and evaluation of novel azoles as potent antifungal agents. |
| AID164105 | Minimum inhibitory concentration against Pseudomonas aeruginosae ATCC 27853 by agar plate dilution method; NT=Not tested | 2004 | Bioorganic & medicinal chemistry letters, Feb-09, Volume: 14, Issue:3 | Synthesis and antifungal activities of phenylenedithioureas. |
| AID1186285 | Inhibition of CYP3A4 in human liver microsome | 2014 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 24, Issue:17 | Discovery of novel pyrimidine and malonamide derivatives as TGR5 agonists. |
| AID1165283 | Inhibition of human CYP3A4 at 10 uM | 2014 | Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20 | Development of (E)-2-((1,4-dimethylpiperazin-2-ylidene)amino)-5-nitro-N-phenylbenzamide, ML336: Novel 2-amidinophenylbenzamides as potent inhibitors of venezuelan equine encephalitis virus. |
| AID532544 | Antifungal activity against wild-type Saccharomyces cerevisiae BY4741 assessed as accumulation of lanosterol at 4 ug/ml (Rvb = 17+/- 1.22 %) | 2008 | Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10 | Differential azole antifungal efficacies contrasted using a Saccharomyces cerevisiae strain humanized for sterol 14 alpha-demethylase at the homologous locus. |
| AID618045 | Antifungal activity against 10'5 CFU/mL Candida albicans MTCC 183 at 100 ug/ml after 48 hrs by disc diffusion technique | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Synthesis and studies of novel 2-(4-cyano-3-trifluoromethylphenyl amino)-4-(quinoline-4-yloxy)-6-(piperazinyl/piperidinyl)-s-triazines as potential antimicrobial, antimycobacterial and anticancer agents. |
| AID1110738 | Antifungal activity against Trichosporon beigelii 1188 after 48 hr by microdilution broth method | 2002 | Farmaco (Societa chimica italiana : 1989), Feb, Volume: 57, Issue:2 | Ring substituted 3-phenyl-1-(2-pyrazinyl)-2-propen-1-ones as potential photosynthesis-inhibiting, antifungal and antimycobacterial agents. |
| AID396960 | Antifungal activity against Fusarium solani NCIM 1330 at 200 ug/disk after 48 hrs by agar disc-diffusion method | 2009 | European journal of medicinal chemistry, May, Volume: 44, Issue:5 | Synthesis, antimicrobial and cytotoxic activities of 1,3,4-oxadiazoles, 1,3,4-thiadiazoles and 1,2,4-triazoles. |
| AID481659 | Antifungal activity against Candida albicans clinical isolate after 24 hrs by broth microdilution assay | 2010 | European journal of medicinal chemistry, May, Volume: 45, Issue:5 | Synthesis and the selective antifungal activity of 5,6,7,8-tetrahydroimidazo[1,2-a]pyridine derivatives. |
| AID574251 | Antifungal activity against 10'8 cells/ml wild-type Candida albicans BF-1 planktonic cells by XTT reduction assay | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | Cell density and cell aging as factors modulating antifungal resistance of Candida albicans biofilms. |
| AID294851 | Antifungal activity against Cryptococcus neoformans ATCC BLS108 after 72 hrs by micro-broth dilution method | 2007 | European journal of medicinal chemistry, Sep, Volume: 42, Issue:9 | Synthesis of novel triazole derivatives as inhibitors of cytochrome P450 14alpha-demethylase (CYP51). |
| AID560137 | Antifungal activity against Candida glabrata isolate 21231 at 10 ug after 48 hrs by disk diffusion method | 2009 | Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7 | Hypersusceptibility to azole antifungals in a clinical isolate of Candida glabrata with reduced aerobic growth. |
| AID1171979 | Antibacterial activity against Micrococcus luteus MTCC 106 assessed as zone of inhibition at 1 mg/disc after 24 hrs by disc diffusion method | 2015 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2 | Facile and diastereoselective synthesis of 3,2'-spiropyrrolidine-oxindoles derivatives, their molecular docking and antiproliferative activities. |
| AID1300883 | Antifungal activity against Candida sake clinical isolate after 24 hrs by broth microdilution method | 2016 | European journal of medicinal chemistry, Jul-19, Volume: 117 | Novel 1,3-thiazolidin-4-one derivatives as promising anti-Candida agents endowed with anti-oxidant and chelating properties. |
| AID645288 | Antifungal activity against Candida albicans NRRL Y-477 at 50 ug/ml after 48 hrs by agar well diffusion method | 2012 | European journal of medicinal chemistry, Apr, Volume: 50 | Regioselective synthesis and antimicrobial activities of some novel aryloxyacetic acid derivatives. |
| AID313549 | Inhibition of hepatic CYP1A2 at 1 uM | 2008 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 18, Issue:1 | Synthesis, biological evaluation and molecular modelling studies of novel ACD- and ABD-ring steroidomimetics as inhibitors of CYP17. |
| AID644193 | Antifungal activity against Aspergillus flavus ATCC 9643 treated for 72 hrs followed by sub-cultivated for 5 days by serial dilution method | 2012 | Bioorganic & medicinal chemistry, Feb-15, Volume: 20, Issue:4 | Synthesis of novel sulfonamide-1,2,4-triazoles, 1,3,4-thiadiazoles and 1,3,4-oxadiazoles, as potential antibacterial and antifungal agents. Biological evaluation and conformational analysis studies. |
| AID39822 | In vitro minimum inhibitory concentration of compound was determined against Aspergillus fumigatus after 48 hr | 2000 | Bioorganic & medicinal chemistry letters, Aug-21, Volume: 10, Issue:16 | 3-Phenyl-5-methyl-2H,5H-furan-2-ones: tuning antifungal activity by varying substituents on the phenyl ring. |
| AID553068 | Inhibition of human recombinant CYP17 expressed in Escherichia coli at 2 uM using progesterone substrate | 2011 | ACS medicinal chemistry letters, Jan-13, Volume: 2, Issue:1 | First Selective CYP11B1 Inhibitors for the Treatment of Cortisol-Dependent Diseases. |
| AID1155712 | Antifungal activity against Penicillium chrysogenum assessed as growth inhibition after 48 hrs by broth dilution method | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Synthesis and antimicrobial activity of amine linked bis- and tris-heterocycles. |
| AID530957 | Antifungal activity against Aspergillus fumigatus ATCC 204305 after 5 days by CLSI method | 2008 | Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7 | Potent in vitro antifungal activities of naturally occurring acetylenic acids. |
| AID644187 | Antifungal activity against Fulvia fulva after 72 hrs by serial dilution method | 2012 | Bioorganic & medicinal chemistry, Feb-15, Volume: 20, Issue:4 | Synthesis of novel sulfonamide-1,2,4-triazoles, 1,3,4-thiadiazoles and 1,3,4-oxadiazoles, as potential antibacterial and antifungal agents. Biological evaluation and conformational analysis studies. |
| AID613258 | Antibacterial activity against Bacillus subtilis ATCC 33712 after 24 hrs by NCCLS M7-A6 broth dilution method | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Design, synthesis and antimicrobial activity of chiral 2-(substituted-hydroxyl)-3-(benzo[d]oxazol-5-yl)propanoic acid derivatives. |
| AID426396 | Inhibition of recombinant CYP3A4 expressed in baculovirus-infected insect microsome | 2009 | European journal of medicinal chemistry, Jul, Volume: 44, Issue:7 | Novel CYP17 inhibitors: synthesis, biological evaluation, structure-activity relationships and modelling of methoxy- and hydroxy-substituted methyleneimidazolyl biphenyls. |
| AID404138 | Antifungal activity against Cryptococcus neoformans H99 | 2005 | Journal of natural products, Nov, Volume: 68, Issue:11 | Extraction, hemisynthesis, and synthesis of canthin-6-one analogues. Evaluation of their antifungal activities. |
| AID636994 | Antifungal activity against Aspergillus niger at 100 ug/disc after 24 hrs by disc diffusion method | 2012 | European journal of medicinal chemistry, Feb, Volume: 48 | Synthesis and biological evaluation of some thiazolidinones as antimicrobial agents. |
| AID1265643 | Antifungal activity against Candida krusei clinical isolate after 24 hrs by sabouraud dextrose broth based microdilution method | 2016 | European journal of medicinal chemistry, Jan-01, Volume: 107 | Anti-Candida activity and cytotoxicity of a large library of new N-substituted-1,3-thiazolidin-4-one derivatives. |
| AID295125 | Antifungal activity against Kluyveromyces fragilis NRRL 2415 at 20 ug after 72 hrs by disk diffusion method | 2007 | European journal of medicinal chemistry, Aug, Volume: 42, Issue:8 | Raman, FT-IR, NMR spectroscopic data and antimicrobial activity of bis[micro2-(benzimidazol-2-yl)-2-ethanethiolato-N,S,S-chloro-palladium(II)] dimer, [(micro2-CH2CH2NHNCC6H4)PdCl]2.C2H5OH complex. |
| AID644190 | Antifungal activity against Trichoderma viride IAM 5061 treated for 72 hrs followed by sub-cultivated for 5 days by serial dilution method | 2012 | Bioorganic & medicinal chemistry, Feb-15, Volume: 20, Issue:4 | Synthesis of novel sulfonamide-1,2,4-triazoles, 1,3,4-thiadiazoles and 1,3,4-oxadiazoles, as potential antibacterial and antifungal agents. Biological evaluation and conformational analysis studies. |
| AID594134 | Antimicrobial activity against Pseudomonas aeruginosa ATCC 27953 after 24 hrs by agar well diffusion method | 2011 | European journal of medicinal chemistry, May, Volume: 46, Issue:5 | Synthesis, antimicrobial, antioxidant, anti-hemolytic and cytotoxic evaluation of new imidazole-based heterocycles. |
| AID55030 | Evaluation of In vitro antifungal activity against Cryptococcus neoformans 87 by broth macro dilution method | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20 | Synthesis and antifungal activity of new azole derivatives containing an N-acylmorpholine ring. |
| AID225405 | Percent decrease in plasma testosterone after 2 hr | 2000 | Journal of medicinal chemistry, Nov-02, Volume: 43, Issue:22 | Synthesis and evaluation of novel steroidal oxime inhibitors of P450 17 (17 alpha-hydroxylase/C17-20-lyase) and 5 alpha-reductase types 1 and 2. |
| AID481661 | Antifungal activity against Candida glabrata clinical isolate 1 after 24 hrs by broth microdilution assay | 2010 | European journal of medicinal chemistry, May, Volume: 45, Issue:5 | Synthesis and the selective antifungal activity of 5,6,7,8-tetrahydroimidazo[1,2-a]pyridine derivatives. |
| AID1304740 | Antifungal activity against Trichophyton rubrum measured after 7 days by serial dilution method | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7 | Discovery of Potent Benzofuran-Derived Diapophytoene Desaturase (CrtN) Inhibitors with Enhanced Oral Bioavailability for the Treatment of Methicillin-Resistant Staphylococcus aureus (MRSA) Infections. |
| AID269148 | Inhibition of rat microsomal 17-alpha-hydroxylase component of P450-17alpha | 2006 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 16, Issue:15 | Synthesis and biochemical evaluation of a range of potent benzyl imidazole-based compounds as potential inhibitors of the enzyme complex 17alpha-hydroxylase/17,20-lyase (P450(17alpha)). |
| AID515182 | Antimicrobial activity against Aspergillus niger CGMCC 3.316 after 48 hrs by modified microdilution method | 2010 | European journal of medicinal chemistry, Oct, Volume: 45, Issue:10 | Synthesis and antimicrobial activities of novel 1H-dibenzo[a,c]carbazoles from dehydroabietic acid. |
| AID1079938 | Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source] | |||
| AID1557088 | Antifungal activity against Candida glabrata 192 assessed as reduction in fungal cell growth incubated for 48 hrs by MTT based broth double dilution method | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Antifungal activity, mode of action variability, and subcellular distribution of coumarin-based antifungal azoles. |
| AID1263196 | Inhibition of rat liver type 1 5alpha-reductase assessed as transformation of testosterone to dihydrotestosterone | 2015 | Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24 | Synthesis and activity of novel 16-dehydropregnenolone acetate derivatives as inhibitors of type 1 5α-reductase and on cancer cell line SK-LU-1. |
| AID632566 | Antifungal activity against Penicillium chrysogenum at 200 ug/mL after 48 hrs by agar cup diffusion assay | 2011 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 21, Issue:24 | A new antifungal briarane diterpenoid from the gorgonian Junceella juncea Pallas. |
| AID632564 | Antifungal activity against Aspergillus niger at 200 ug/mL after 48 hrs by agar cup diffusion assay | 2011 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 21, Issue:24 | A new antifungal briarane diterpenoid from the gorgonian Junceella juncea Pallas. |
| AID49129 | In vitro Minimum lethal concentration was determined by microbroth dilution assay on Candida albicans | 1992 | Journal of medicinal chemistry, Jan, Volume: 35, Issue:1 | Synthesis, specificity, and antifungal activity of inhibitors of the Candida albicans delta 24-sterol methyltransferase. |
| AID50131 | In vitro evaluation of minimum inhibitory concentration against Candida guilliermondii 26 | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20 | Synthesis and antifungal activity of new azole derivatives containing an N-acylmorpholine ring. |
| AID322755 | Binding affinity to human CYP51 | 2007 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 35, Issue:3 | Three-dimensional quantitative structure-activity relationship analysis of human CYP51 inhibitors. |
| AID405113 | Antimicrobial activity against Apophysomyces elegans assessed as percent of susceptible isolates after 24 hrs | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | In vitro susceptibilities of 217 clinical isolates of zygomycetes to conventional and new antifungal agents. |
| AID1467466 | Antifungal activity against Fusarium moniliforme at 25 ug/ml after 48 hrs by agar well diffusion method | 2017 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 27, Issue:14 | Synthesis, SAR and molecular docking studies of benzo[d]thiazole-hydrazones as potential antibacterial and antifungal agents. |
| AID530941 | Antifungal activity against Trichophyton rubrum ATCC 10218 by CLSI method | 2008 | Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7 | Potent in vitro antifungal activities of naturally occurring acetylenic acids. |
| AID287382 | Antifungal activity against Rhodotorula rubra after 24 hrs by disk diffusion method | 2007 | European journal of medicinal chemistry, Feb, Volume: 42, Issue:2 | Synthesis, characterization and antimicrobial activity of Fe(II), Zn(II), Cd(II) and Hg(II) complexes with 2,6-bis(benzimidazol-2-yl) pyridine ligand. |
| AID1328093 | Antifungal activity against Penicillium chrysogenum assessed as inhibition of spore germination after 48 hrs by broth dilution method | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | Synthesis and antimicrobial activity of styryl/pyrrolyl/pyrazolyl sulfonylmethyl-1,3,4-oxadiazolyl amines and styryl/pyrrolyl/pyrazolyl sulfonylmethyl-1,3,4-thiadiazolyl amines. |
| AID681127 | TP_TRANSPORTER: inhibition of LDS-751 efflux in NIH-3T3-G185 cells | 2001 | Biochemical and biophysical research communications, Nov-30, Volume: 289, Issue:2 | Active transport of fluorescent P-glycoprotein substrates: evaluation as markers and interaction with inhibitors. |
| AID49974 | In vitro minimum inhibitory concentration of compound was determined against Candida glabrata after 48 hr | 2000 | Bioorganic & medicinal chemistry letters, Aug-21, Volume: 10, Issue:16 | 3-Phenyl-5-methyl-2H,5H-furan-2-ones: tuning antifungal activity by varying substituents on the phenyl ring. |
| AID490991 | Antifungal activity against Fusarium solani at 100 ug/disk after 48 hrs by disk diffusion method | 2010 | European journal of medicinal chemistry, Jul, Volume: 45, Issue:7 | Synthesis and bioassay of pyrrolyl oxazolines and thiazolines. |
| AID407007 | Antimicrobial activity against Candida albicans FH1 intact biofilms after 48 hrs by XTT assay | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | Role for cell density in antifungal drug resistance in Candida albicans biofilms. |
| AID53376 | Inhibition of C17,20-lyase enzyme, cytochrome P450 17A1 in Human testicular microsomes | 1996 | Journal of medicinal chemistry, Aug-16, Volume: 39, Issue:17 | 3- and 4-pyridylalkyl adamantanecarboxylates: inhibitors of human cytochrome P450(17 alpha) (17 alpha-hydroxylase/C17,20-lyase). Potential nonsteroidal agents for the treatment of prostatic cancer. |
| AID1301342 | Inhibition of CYP3A4 (unknown origin) at 20 uM by P450-glo assay | 2016 | Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13 | Novel free fatty acid receptor 1 (GPR40) agonists based on 1,3,4-thiadiazole-2-carboxamide scaffold. |
| AID322156 | Antifungal activity against Candida albicans C 128-2000 after 48 hrs by CLSI M27-A2 method | 2008 | Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1 | N-Phenyl and N-phenylalkyl-maleimides acting against Candida spp.: time-to-kill, stability, interaction with maleamic acids. |
| AID242797 | In vitro inhibitory concentration against human CYP11B1 expressed in V79 MZh hamster fibroblasts incubated with 100 nM of substrate deoxy-corticosterone in presence of the compound | 2005 | Journal of medicinal chemistry, Mar-10, Volume: 48, Issue:5 | Synthesis and evaluation of (pyridylmethylene)tetrahydronaphthalenes/-indanes and structurally modified derivatives: potent and selective inhibitors of aldosterone synthase. |
| AID1129515 | Antimicrobial activity against Pseudomonas aeruginosa ATCC 27853 after 24 hrs by broth dilution method | 2014 | European journal of medicinal chemistry, Apr-22, Volume: 77 | Synthesis, antimicrobial and cytotoxic activities of pyrimidinyl benzoxazole, benzothiazole and benzimidazole. |
| AID456683 | Antifungal activity against Cryptococcus neoformans ATCC 32264 assessed as inhibition of fungal growth at 50 uM after 48 hrs by microbroth dilution method | 2010 | Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1 | New small-size peptides possessing antifungal activity. |
| AID572692 | Binding affinity to Mycobacterium smegmatis ATCC 700084 CYP51 at pH7.5 | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | Identification, characterization, and azole-binding properties of Mycobacterium smegmatis CYP164A2, a homolog of ML2088, the sole cytochrome P450 gene of Mycobacterium leprae. |
| AID362913 | Antifungal activity against Candida albicans after 24 hrs by broth microdilution method | 2008 | Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17 | NO-donors. Part 17: Synthesis and antimicrobial activity of novel ketoconazole-NO-donor hybrid compounds. |
| AID1068771 | Antifungal activity against Aspergillus niger after 48 hrs by broth dilution test | 2014 | European journal of medicinal chemistry, Feb-12, Volume: 73 | Synthesis and antimicrobial activity of (1,4-phenylene)bis(arylsulfonylpyrazoles and isoxazoles). |
| AID397012 | Antifungal activity against Aspergillus niger 5021 after 48 hrs by microplate alamar blue assay | 2009 | European journal of medicinal chemistry, May, Volume: 44, Issue:5 | Synthesis, antimicrobial evaluation and QSAR study of some 3-hydroxypyridine-4-one and 3-hydroxypyran-4-one derivatives. |
| AID515011 | Antifungal activity against Candida parapsilosis by micro-broth dilution method | 2010 | European journal of medicinal chemistry, Oct, Volume: 45, Issue:10 | Synthesis and antifungal evaluation of novel triazole derivatives as inhibitors of cytochrome P450 14alpha-demethylase. |
| AID723708 | Antifungal activity against Aspergillus fumigatus after 72 hrs by serial dilution technique | 2013 | Bioorganic & medicinal chemistry, Jan-15, Volume: 21, Issue:2 | Synthesis and biological evaluation of some 5-arylidene-2-(1,3-thiazol-2-ylimino)-1,3-thiazolidin-4-ones as dual anti-inflammatory/antimicrobial agents. |
| AID242435 | Displacement of [3H]R-1881 from Androgen receptor of LNCaP cells; - = not determined | 2005 | Journal of medicinal chemistry, Apr-21, Volume: 48, Issue:8 | Novel C-17-heteroaryl steroidal CYP17 inhibitors/antiandrogens: synthesis, in vitro biological activity, pharmacokinetics, and antitumor activity in the LAPC4 human prostate cancer xenograft model. |
| AID1456582 | Antifungal activity against Trichophyton rubrum isolate cmccftla by micro-broth dilution method | 2017 | Bioorganic & medicinal chemistry letters, 05-15, Volume: 27, Issue:10 | Design, synthesis, and in vitro evaluation of novel antifungal triazoles. |
| AID131260 | Tested for efficacy of compound in experimental systemic candidosis (mouse) after oral treatment at dosage of 8 *200 mg kg e-1 | 1994 | Journal of medicinal chemistry, Jun-24, Volume: 37, Issue:13 | Derivatives of a novel cyclopeptolide. 1. Synthesis, antifungal activity, and structure-activity relationships. |
| AID449684 | Antifungal activity against Fusarium solani NCIM 1330 at 100 ug/disk after 48 hrs by agar disk diffusion method | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11 | Synthesis, antimicrobial and antioxidant activities of substituted pyrazoles, isoxazoles, pyrimidine and thioxopyrimidine derivatives. |
| AID204343 | In vitro antifungal activity against Sporothrix schenck ii | 1984 | Journal of medicinal chemistry, Jul, Volume: 27, Issue:7 | Antimycotic azoles. 7. Synthesis and antifungal properties of a series of novel triazol-3-ones. |
| AID625284 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID468471 | Antimicrobial activity against Candida albicans ATCC 18804 after 48 hrs | 2010 | European journal of medicinal chemistry, Mar, Volume: 45, Issue:3 | Synthesis, characterization and biocidal activity of new organotin complexes of 2-(3-oxocyclohex-1-enyl)benzoic acid. |
| AID532533 | Antifungal activity against Saccharomyces cerevisiae BY4741 harboring human CYP51 assessed as accumulation of lanosterol at 4 ug/ml (Rvb = 23+/- 1.08 %) | 2008 | Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10 | Differential azole antifungal efficacies contrasted using a Saccharomyces cerevisiae strain humanized for sterol 14 alpha-demethylase at the homologous locus. |
| AID407002 | Antimicrobial activity against Candida albicans GDH2346 intact biofilms after 48 hrs by XTT assay | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | Role for cell density in antifungal drug resistance in Candida albicans biofilms. |
| AID596447 | Antifungal activity against Aspergillus fumigatus ATCC 26934 | 2011 | Bioorganic & medicinal chemistry, May-01, Volume: 19, Issue:9 | Antifungal, cytotoxic and SAR studies of a series of N-alkyl, N-aryl and N-alkylphenyl-1,4-pyrrolediones and related compounds. |
| AID290150 | Antifungal activity against Trichophyton rubrum after 48 hrs by MTT colorimetric method | 2007 | European journal of medicinal chemistry, Apr, Volume: 42, Issue:4 | Synthesis and antimicrobial activities of Schiff bases derived from 5-chloro-salicylaldehyde. |
| AID50140 | Evaluation of In vitro antifungal activity against Candida krusei 70 by broth macro dilution method | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20 | Synthesis and antifungal activity of new azole derivatives containing an N-acylmorpholine ring. |
| AID376219 | Antifungal activity against Candida glabrata after 24 hrs | 2000 | Journal of natural products, Jul, Volume: 63, Issue:7 | New caryophyllene derivatives from Betula litwinowii. |
| AID322163 | Antifungal activity against Candida krusei C 117-2000 after 48 hrs by CLSI M27-A2 method | 2008 | Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1 | N-Phenyl and N-phenylalkyl-maleimides acting against Candida spp.: time-to-kill, stability, interaction with maleamic acids. |
| AID1176161 | Inhibition of human recombinant MDR1 in cell membrane fraction preincubated for 5 mins at 10 uM measured after 40 mins by Pgp-Glo luciferase assay | 2015 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2 | Investigating the binding interactions of the anti-Alzheimer's drug donepezil with CYP3A4 and P-glycoprotein. |
| AID586580 | Inhibition of human CYP17 expressed in Escherichia coli using progesterone as a substrate | 2011 | Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6 | Design, synthesis, and biological evaluation of imidazolyl derivatives of 4,7-disubstituted coumarins as aromatase inhibitors selective over 17-α-hydroxylase/C17-20 lyase. |
| AID635005 | Antifungal activity against Fusarium solani NCIM 1330 assessed as zone of inhibition at 200 ug/disc after 48 hrs by disk diffusion method | 2012 | European journal of medicinal chemistry, Jan, Volume: 47, Issue:1 | Synthesis, antimicrobial, antimycobacterial and structure-activity relationship of substituted pyrazolo-, isoxazolo-, pyrimido- and mercaptopyrimidocyclohepta[b]indoles. |
| AID566958 | Antifungal activity against Cryptococcus neoformans ATCC 32264 assessed as inhibition of fungal growth at 6.25 uM after 48 hrs by microplate analysis | 2011 | European journal of medicinal chemistry, Jan, Volume: 46, Issue:1 | Penetratin analogues acting as antifungal agents. |
| AID1196736 | Antifungal activity against Candida krusei NRLL Y 7179 after 48 hrs by broth microdilution assay | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | A novel series of thiazolyl-pyrazoline derivatives: synthesis and evaluation of antifungal activity, cytotoxicity and genotoxicity. |
| AID315657 | Inhibition of recombinant CYP1A2 at 1 uM | 2008 | Bioorganic & medicinal chemistry, Feb-15, Volume: 16, Issue:4 | Synthesis, biological evaluation and molecular modelling studies of methyleneimidazole substituted biaryls as inhibitors of human 17alpha-hydroxylase-17,20-lyase (CYP17). Part I: Heterocyclic modifications of the core structure. |
| AID370296 | Effect on CYP3A4 in human liver assessed as testosterone 6-beta-hydroxylation at 100 uM relative to control | 2006 | PLoS medicine, Nov, Volume: 3, Issue:11 | OPC-67683, a nitro-dihydro-imidazooxazole derivative with promising action against tuberculosis in vitro and in mice. |
| AID106801 | Inhibition of malate dehydrogenase (MDH) | 2003 | Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21 | Identification and prediction of promiscuous aggregating inhibitors among known drugs. |
| AID213652 | 50% inhibitory concentration against the growth of Trypanosoma cruzi (Epimastigotes) | 2000 | Journal of medicinal chemistry, May-04, Volume: 43, Issue:9 | Design and synthesis of aryloxyethyl thiocyanate derivatives as potent inhibitors of Trypanosoma cruzi proliferation. |
| AID530953 | Antifungal activity against Trichophyton mentagrophytes ATCC MYA-4439 by CLSI method | 2008 | Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7 | Potent in vitro antifungal activities of naturally occurring acetylenic acids. |
| AID1104306 | Antifungal activity against Penicillium ochrochloron ATCC 9112 at 28 degC measured after 72 hr by microdilution method | 2010 | Chemical & pharmaceutical bulletin, Feb, Volume: 58, Issue:2 | Sulfonamide-1,2,4-thiadiazole derivatives as antifungal and antibacterial agents: synthesis, biological evaluation, lipophilicity, and conformational studies. |
| AID221163 | Inhibition of lanosterol 14-alpha-demethylase of rat hepatic microsomes | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | Selective inhibition of mammalian lanosterol 14 alpha-demethylase: a possible strategy for cholesterol lowering. |
| AID389818 | Inhibition of human recombinant CYP3A4 expressed in baculovirus-infected insect microsomes | 2008 | Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24 | In vivo active aldosterone synthase inhibitors with improved selectivity: lead optimization providing a series of pyridine substituted 3,4-dihydro-1H-quinolin-2-one derivatives. |
| AID696544 | Antifungal activity against Trichophyton rubrum CCC 113 after 48 hrs by broth microdilution technique | 2012 | Bioorganic & medicinal chemistry, Nov-01, Volume: 20, Issue:21 | Synthesis and antifungal activity of diverse C-2 pyridinyl and pyridinylvinyl substituted quinolines. |
| AID549048 | Antifungal activity against Candida albicans CA127 after 48 hrs by broth microdilution method | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | In vitro activities of retigeric acid B alone and in combination with azole antifungal agents against Candida albicans. |
| AID1265642 | Antifungal activity against Candida tropicalis clinical isolate after 24 hrs by sabouraud dextrose broth based microdilution method | 2016 | European journal of medicinal chemistry, Jan-01, Volume: 107 | Anti-Candida activity and cytotoxicity of a large library of new N-substituted-1,3-thiazolidin-4-one derivatives. |
| AID1218832 | Inactivation of recombinant CYP3A4 (unknown origin) using testosterone as substrate assessed as recovery of enzyme activity at 1 uM preincubated for 5 mins followed by dialysis measured after 24 hrs | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7 | Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme. |
| AID625285 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID334239 | Antimicrobial activity against Cladosporium cladosporioides IMI 299104 after 10 days by microdilution technique | 2002 | Journal of natural products, Apr, Volume: 65, Issue:4 | Antimicrobial activities of a new schizozygane indoline alkaloid from Schizozygia coffaeoides and the revised structure of isoschizogaline. |
| AID407018 | Antimicrobial activity against Chk1 deficient Candida albicans CHK21 at planktonic cell density of 10'3 cells/ml after 48 hrs by XTT assay | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | Role for cell density in antifungal drug resistance in Candida albicans biofilms. |
| AID45327 | Evaluation of In vitro antifungal activity against Candida albicans 76 by broth macro dilution method | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20 | Synthesis and antifungal activity of new azole derivatives containing an N-acylmorpholine ring. |
| AID89415 | Inhibition of cellular cholesterol biosynthesis using human fibroblasts in tissue culture | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | Selective inhibition of mammalian lanosterol 14 alpha-demethylase: a possible strategy for cholesterol lowering. |
| AID1072932 | Inhibition of CYP3A4 (unknown origin) at 10 uM relative to control | 2014 | ACS medicinal chemistry letters, Mar-13, Volume: 5, Issue:3 | Potent Hepatitis C Virus NS5A Inhibitors Containing a Benzidine Core. |
| AID1328455 | Half life in Hartley guinea pig liver microsomes in presence of NADPH by LC-MS/MS analysis | 2016 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 26, Issue:23 | Design, synthesis, and evaluation of (2S,4R)-Ketoconazole sulfonamide analogs as potential treatments for Metabolic Syndrome. |
| AID1129510 | Antimicrobial activity against Penicillium chrysogenum at 25 ug/well after 48 hrs by agar well diffusion method | 2014 | European journal of medicinal chemistry, Apr-22, Volume: 77 | Synthesis, antimicrobial and cytotoxic activities of pyrimidinyl benzoxazole, benzothiazole and benzimidazole. |
| AID1328453 | Inhibition of human Cyp3A4 using testosterone as substrate by LC-MS/MS analysis | 2016 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 26, Issue:23 | Design, synthesis, and evaluation of (2S,4R)-Ketoconazole sulfonamide analogs as potential treatments for Metabolic Syndrome. |
| AID364065 | Antifungal activity against Aspergillus niger ATCC 16404 after 48 hrs by MTT assay | 2008 | European journal of medicinal chemistry, Sep, Volume: 43, Issue:9 | Enamines as novel antibacterials and their structure-activity relationships. |
| AID524793 | Antiplasmodial activity against Plasmodium falciparum Dd2 after 72 hrs by SYBR green assay | 2009 | Nature chemical biology, Oct, Volume: 5, Issue:10 | Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum. |
| AID1557091 | Cytotoxicity against human HEK293T cells assessed as reduction in cell viability at 5 to 50 uM incubated for 24 hrs by XTT assay | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Antifungal activity, mode of action variability, and subcellular distribution of coumarin-based antifungal azoles. |
| AID574268 | Antifungal activity against 24 hrs cultures of 10'7 cells/ml biofilm-derived Candida albicans BF-1 planktonic cells hrs by XTT reduction method | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | Cell density and cell aging as factors modulating antifungal resistance of Candida albicans biofilms. |
| AID48233 | In vitro evaluation of minimum inhibitory concentration against Candida pseudotropicalis 13 | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20 | Synthesis and antifungal activity of new azole derivatives containing an N-acylmorpholine ring. |
| AID733697 | Antifungal activity against Candida albicans MTCC 227 after 48 to 72 hrs | 2013 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6 | Facile one-pot synthesis of novel dispirooxindole-pyrrolidine derivatives and their antimicrobial and anticancer activity against A549 human lung adenocarcinoma cancer cell line. |
| AID86931 | Percentage lowering of the total serum cholesterol in male hamsters at a dose of 200 mg/dL orally administered for 14 days | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | Selective inhibition of mammalian lanosterol 14 alpha-demethylase: a possible strategy for cholesterol lowering. |
| AID574261 | Antifungal activity against 48 hrs cultures of 10'7 cells/ml Candida albicans ATCC 90028 planktonic cells by XTT reduction method | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | Cell density and cell aging as factors modulating antifungal resistance of Candida albicans biofilms. |
| AID39835 | Minimum inhibitory concentration of compound for antifungal activity against Aspergillus fumigatus | 2000 | Bioorganic & medicinal chemistry letters, Oct-02, Volume: 10, Issue:19 | Novel antifungals based on 4-substituted imidazole: a combinatorial chemistry approach to lead discovery and optimization. |
| AID733707 | Antifungal activity against Candida albicans MTCC 227 at 1 mg/disc after 48 hrs by disc diffusion method | 2013 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6 | Facile one-pot synthesis of novel dispirooxindole-pyrrolidine derivatives and their antimicrobial and anticancer activity against A549 human lung adenocarcinoma cancer cell line. |
| AID555135 | Antimicrobial activity against Candida albicans by EUCAST broth microdilution method | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Fenticonazole activity measured by the methods of the European Committee on Antimicrobial Susceptibility Testing and CLSI against 260 Candida vulvovaginitis isolates from two European regions and annotations on the prevalent genotypes. |
| AID1332949 | Antifungal activity against Aspergillus flavus MTCC 1884 measured after 2 days by broth dilution method | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Synthesis, antimicrobial activity and advances in structure-activity relationships (SARs) of novel tri-substituted thiazole derivatives. |
| AID420070 | Antifungal activity against Candida krusei after 24 hrs by broth microdilution assay | 2009 | Bioorganic & medicinal chemistry, Jun-01, Volume: 17, Issue:11 | Bulky 1,4-benzoxazine derivatives with antifungal activity. |
| AID48947 | Tested for minimum inhibitory concentration against Candida albicans 9 (Candida albicans) at pH 6.5. | 1994 | Journal of medicinal chemistry, Jun-24, Volume: 37, Issue:13 | Derivatives of a novel cyclopeptolide. 1. Synthesis, antifungal activity, and structure-activity relationships. |
| AID1061742 | Antimicrobial activity against Candida albicans SC5314 after 24 hrs by broth microdilution method | 2014 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1 | Synthesis and evaluation of novel azoles as potent antifungal agents. |
| AID1176152 | Inhibition of human recombinant CYP3A4 expressed in insect cell microsomes preincubated for 10 mins at 1 uM by fluorescence assay | 2015 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2 | Investigating the binding interactions of the anti-Alzheimer's drug donepezil with CYP3A4 and P-glycoprotein. |
| AID207272 | Inhibition of Steroid 17-alpha-hydroxylase/17,20 lyase cytochrome P450 17A1 | 1992 | Journal of medicinal chemistry, Jul-24, Volume: 35, Issue:15 | Stereoisomers of ketoconazole: preparation and biological activity. |
| AID209250 | Minimum inhibitory concentration against Streptococcus faecalis ATCC 29212 by agar plate dilution method; NT=Not tested | 2004 | Bioorganic & medicinal chemistry letters, Feb-09, Volume: 14, Issue:3 | Synthesis and antifungal activities of phenylenedithioureas. |
| AID367159 | Antimicrobial activity against Sporothrix schenckii by broth microdilution method | 2009 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 19, Issue:3 | Synthesis and antifungal activity of 1,2,3-triazole containing fluconazole analogues. |
| AID42882 | Inhibition of Candida lusitaniae 2446/I growth for 24 hours in vitro. | 2001 | Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17 | 3-Phenyl-5-acyloxymethyl-2H,5H-furan-2-ones: synthesis and biological activity of a novel group of potential antifungal drugs. |
| AID1176158 | Inhibition of human recombinant MDR1 in cell membrane fraction preincubated for 5 mins at 0.01 uM measured after 40 mins by Pgp-Glo luciferase assay | 2015 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2 | Investigating the binding interactions of the anti-Alzheimer's drug donepezil with CYP3A4 and P-glycoprotein. |
| AID428318 | Inhibition of P-gp in human Caco-2 cells assessed as increase in influx permeability from apical to basolateral side at 50 uM after 120 mins | 2009 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15 | Synthesis and antimultidrug resistance evaluation of icariin and its derivatives. |
| AID405103 | Antimicrobial activity against Rhizopus sp. assessed as percent of susceptible isolates after 24 hrs | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | In vitro susceptibilities of 217 clinical isolates of zygomycetes to conventional and new antifungal agents. |
| AID1307792 | Inhibition of CYP3A4 in human liver microsomes using midazolam as substrate after 4 mins by LC-MS analysis | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7 | Understanding Oxadiazolothiazinone Biological Properties: Negative Inotropic Activity versus Cytochrome P450-Mediated Metabolism. |
| AID1079935 | Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source] | |||
| AID363710 | Antifungal activity against Candida albicans ATCC 10231 after 48 hrs by broth microdilution technique | 2008 | Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17 | In vitro antifungal activity of polyfunctionalized 2-(hetero)arylquinolines prepared through imino Diels-Alder reactions. |
| AID207276 | Percent inhibition of Steroid 17-alpha-hydroxylase/17,20 lyase from rat testes microsomes at 100 uM | 1990 | Journal of medicinal chemistry, Sep, Volume: 33, Issue:9 | Hydroxyperfluoroazobenzenes: novel inhibitors of enzymes of androgen biosynthesis. |
| AID1244279 | Inhibition of CYP3A4 (unknown origin) | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | 4-Fluoro-3',4',5'-trimethoxychalcone as a new anti-invasive agent. From discovery to initial validation in an in vivo metastasis model. |
| AID1467467 | Antifungal activity against Fusarium moniliforme at 50 ug/ml after 48 hrs by agar well diffusion method | 2017 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 27, Issue:14 | Synthesis, SAR and molecular docking studies of benzo[d]thiazole-hydrazones as potential antibacterial and antifungal agents. |
| AID611679 | Antibacterial activity against Bacillus megaterium at 0.05 mg by agar diffusion method | 2011 | Journal of natural products, Jul-22, Volume: 74, Issue:7 | Bioactive 11,20-epoxy-3,5(16)-diene briarane diterpenoids from the South China Sea gorgonian Dichotella gemmacea. |
| AID1157290 | Antifungal activity against Candida albicans Y0109 assessed as growth inhibition by automatic microplate reader analysis | 2014 | Journal of natural products, May-23, Volume: 77, Issue:5 | Polyhydroxy cyclohexanols from a Dendrodochium sp. fungus associated with the sea cucumber Holothuria nobilis Selenka. |
| AID374104 | Antimicrobial activity against Aspergillus fumigatus ATCC 96918 at 100 ug/disk after 5 days by agar disk diffusion method | 2009 | European journal of medicinal chemistry, Apr, Volume: 44, Issue:4 | New acyclic nucleosides analogues as potential analgesic, anti-inflammatory, anti-oxidant and anti-microbial derived from pyrimido[4,5-b]quinolines. |
| AID287722 | Inhibition of human recombinant aromatase at 3 uM after 30 mins relative to control | 2007 | Bioorganic & medicinal chemistry, Apr-01, Volume: 15, Issue:7 | Synthesis of DL-standishinal and its related compounds for the studies on structure-activity relationship of inhibitory activity against aromatase. |
| AID53384 | Inhibition of human testicular microsomal cytochrome P450 17A1 | 1998 | Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6 | Novel 17-azolyl steroids, potent inhibitors of human cytochrome 17 alpha-hydroxylase-C17,20-lyase (P450(17) alpha): potential agents for the treatment of prostate cancer. |
| AID717023 | Antifungal activity against Candida albicans ATCC 10231 after 24 hrs by microdilution susceptibility assay | 2012 | European journal of medicinal chemistry, Dec, Volume: 58 | Synthesis and biological evaluation of some hydrazone derivatives as new anticandidal and anticancer agents. |
| AID50137 | Minimum inhibitory concentration of compound for antifungal activity against Candida kefyr | 2000 | Bioorganic & medicinal chemistry letters, Oct-02, Volume: 10, Issue:19 | Novel antifungals based on 4-substituted imidazole: a combinatorial chemistry approach to lead discovery and optimization. |
| AID619213 | Antifungal activity against 10'5 CFU/mL Aspergillus fumigatus MTCC 343 after 48 hrs by agar streak dilution method | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Synthesis and studies of novel 2-(4-cyano-3-trifluoromethylphenyl amino)-4-(quinoline-4-yloxy)-6-(piperazinyl/piperidinyl)-s-triazines as potential antimicrobial, antimycobacterial and anticancer agents. |
| AID207140 | Inhibition of human testicular microsome Steroid 17-alpha-hydroxylase/17,20 lyase | 2001 | Journal of medicinal chemistry, Mar-01, Volume: 44, Issue:5 | A new class of nonsteroidal aromatase inhibitors: design and synthesis of chromone and xanthone derivatives and inhibition of the P450 enzymes aromatase and 17 alpha-hydroxylase/C17,20-lyase. |
| AID419387 | Antifungal activity against Aspergillus niger ATCC 9029 at 100 ug/disk after 48 hrs by paper disk diffusion technique | 2009 | European journal of medicinal chemistry, May, Volume: 44, Issue:5 | Synthesis and anti-microbial screening of some Schiff bases of 3-amino-6,8-dibromo-2-phenylquinazolin-4(3H)-ones. |
| AID481669 | Cytotoxicity against human SK-MEL cells up to 25 ug/ml after 48 hrs by neutral red assay | 2010 | European journal of medicinal chemistry, May, Volume: 45, Issue:5 | Synthesis and the selective antifungal activity of 5,6,7,8-tetrahydroimidazo[1,2-a]pyridine derivatives. |
| AID394828 | Inhibition of human recombinant CYP3A4 | 2009 | Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6 | Rational modification of a candidate cancer drug for use against Chagas disease. |
| AID228069 | In vivo activity against microsporosis guinea pig, measured as the ratio of animals cured/animals infected (C/I) at dose 2.5 mg/kg;0/14 | 1984 | Journal of medicinal chemistry, Jul, Volume: 27, Issue:7 | Antimycotic azoles. 7. Synthesis and antifungal properties of a series of novel triazol-3-ones. |
| AID376047 | Antifungal activity against Trichophyton rubrum C 113 by agar dilution method | 1999 | Journal of natural products, Oct, Volume: 62, Issue:10 | In vitro evaluation of antifungal properties of phenylpropanoids and related compounds acting against dermatophytes. |
| AID1557089 | Inhibition of recombinant human CYP3A4 using Luciferin-PPXE as substrate preincubated for 10 mins followed by NADPH addition measured after 15 mins by luminometric method | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Antifungal activity, mode of action variability, and subcellular distribution of coumarin-based antifungal azoles. |
| AID244022 | Inhibition of [1-beta-3H]-androstenedione binding to human steroid 5-alpha-reductase type I expressed in DU-145 cells at 10 uM; - = not determined | 2005 | Journal of medicinal chemistry, Apr-21, Volume: 48, Issue:8 | Novel C-17-heteroaryl steroidal CYP17 inhibitors/antiandrogens: synthesis, in vitro biological activity, pharmacokinetics, and antitumor activity in the LAPC4 human prostate cancer xenograft model. |
| AID1451800 | Antifungal activity against Trichophyton verrucosum after 7 days | 2017 | Journal of medicinal chemistry, 10-12, Volume: 60, Issue:19 | Novel Inhibitors of Staphyloxanthin Virulence Factor in Comparison with Linezolid and Vancomycin versus Methicillin-Resistant, Linezolid-Resistant, and Vancomycin-Intermediate Staphylococcus aureus Infections in Vivo. |
| AID496828 | Antimicrobial activity against Leishmania donovani | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
| AID491984 | Inhibition of human CYP17 expressed in Escherichia coli coexpressing NADPH-P450 reductase | 2010 | Journal of medicinal chemistry, Jul-08, Volume: 53, Issue:13 | Isopropylidene substitution increases activity and selectivity of biphenylmethylene 4-pyridine type CYP17 inhibitors. |
| AID681126 | TP_TRANSPORTER: inhibition of Rhodamine 123 efflux in NIH-3T3-G185 cells | 2001 | Biochemical and biophysical research communications, Nov-30, Volume: 289, Issue:2 | Active transport of fluorescent P-glycoprotein substrates: evaluation as markers and interaction with inhibitors. |
| AID655580 | Antifungal activity against Candida albicans SC5314 after 24 hrs by microbroth dilution method | 2012 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8 | New triazole derivatives as antifungal agents: synthesis via click reaction, in vitro evaluation and molecular docking studies. |
| AID48925 | Tested In vitro for antifungal activity at pH 5.8 | 2002 | Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13 | Antifungal agents. 10. New derivatives of 1-[(aryl)[4-aryl-1H-pyrrol-3-yl]methyl]-1H-imidazole, synthesis, anti-candida activity, and quantitative structure-analysis relationship studies. |
| AID600687 | Antifungal activity against Aspergillus ochraceus ATCC 12066 after 72 hrs by serial dilution method | 2011 | Bioorganic & medicinal chemistry, May-15, Volume: 19, Issue:10 | Thiazole-based chalcones as potent antimicrobial agents. Synthesis and biological evaluation. |
| AID456834 | Antifungal activity against Penicillium funiculosum ATCC 36839 after 72 hrs by serial dilution method | 2010 | Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1 | Novel 4-thiazolidinone derivatives as potential antifungal and antibacterial drugs. |
| AID211467 | Evaluation of In vitro antifungal activity against Torulopsis glabrata 78 by broth macro dilution method | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20 | Synthesis and antifungal activity of new azole derivatives containing an N-acylmorpholine ring. |
| AID367166 | Cytotoxicity against human Hep3B cells at 1 mg/ml | 2009 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 19, Issue:3 | Synthesis and antifungal activity of 1,2,3-triazole containing fluconazole analogues. |
| AID659901 | Antifungal activity against Candida albicans NRRL Y-477 at 50 ug/ml after 24 hrs by agar well diffusion assay | 2012 | European journal of medicinal chemistry, Jun, Volume: 52 | Design and synthesis of new 4-pyrazolin-3-yl-1,2,3-triazoles and 1,2,3-triazol-4-yl-pyrazolin-1-ylthiazoles as potential antimicrobial agents. |
| AID416041 | Fungicidal activity against tebuconazole-adapted wild type Colletotrichum graminicola CgM2 assessed as inhibition of radial growth rate at 23 degC in darkness | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10 | Treatment of a clinically relevant plant-pathogenic fungus with an agricultural azole causes cross-resistance to medical azoles and potentiates caspofungin efficacy. |
| AID32563 | In vitro minimum inhibitory concentration of compound was determined against Absidia corymbifera after 24 hr r | 2000 | Bioorganic & medicinal chemistry letters, Aug-21, Volume: 10, Issue:16 | 3-Phenyl-5-methyl-2H,5H-furan-2-ones: tuning antifungal activity by varying substituents on the phenyl ring. |
| AID1171996 | Antifungal activity against Malassezia pachydermatis assessed as inhibition of visual growth after 48 to 72 hrs | 2015 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2 | Facile and diastereoselective synthesis of 3,2'-spiropyrrolidine-oxindoles derivatives, their molecular docking and antiproliferative activities. |
| AID242646 | In vitro inhibitory concentration against human placental cytochrome P450 19 with 2.5 uM testosterone; nd= not determined | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Synthesis and evaluation of imidazolylmethylenetetrahydronaphthalenes and imidazolylmethyleneindanes: potent inhibitors of aldosterone synthase. |
| AID313552 | Inhibition of hepatic CYP2C9 at 10 uM | 2008 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 18, Issue:1 | Synthesis, biological evaluation and molecular modelling studies of novel ACD- and ABD-ring steroidomimetics as inhibitors of CYP17. |
| AID39858 | The compound was tested for antifungal activity against Aspergillus fumigatus MF4839 using agar dilution assay | 1987 | Journal of medicinal chemistry, Aug, Volume: 30, Issue:8 | Lysosomotropic agents. 7. Broad-spectrum antifungal activity of lysosomotropic detergents. |
| AID448513 | Antimicrobial activity against Aspergillus fumigatus at 30 ug/mL after 16 to 20 hrs by disk diffusion method | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11 | Synthesis of some novel pyrazolo[3,4-b]pyridine and pyrazolo[3,4-d]pyrimidine derivatives bearing 5,6-diphenyl-1,2,4-triazine moiety as potential antimicrobial agents. |
| AID678717 | Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-benzyloxyquinoline as substrate after 30 mins | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
| AID454780 | Antifungal activity against Microsporum gypseum C 115 after 48 hrs by broth microdilution technique | 2009 | Bioorganic & medicinal chemistry, Nov-01, Volume: 17, Issue:21 | 5-Nitrofuranes and 5-nitrothiophenes with anti-Trypanosoma cruzi activity and ability to accumulate squalene. |
| AID419358 | Antifungal activity against Aspergillus niger at 200 ug/disk after 48 hrs by agar disc-diffusion method | 2009 | European journal of medicinal chemistry, May, Volume: 44, Issue:5 | Synthesis and bioassay of a new class of heterocycles pyrrolyl oxadiazoles/thiadiazoles/triazoles. |
| AID1486357 | Inhibition of MBP-tagged human CYP24A1 expressed Escherichia coli BL21-Gold(DE3) incubated for 25 mins in presence of Adx, AdR 1,25(OH)2D3 and NADPH by HPLC method | 2017 | Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15 | Synthesis, molecular modelling and CYP24A1 inhibitory activity of novel of (E)-N-(2-(1H-imidazol-1-yl)-2-(phenylethyl)-3/4-styrylbenzamides. |
| AID380256 | Antifungal activity against Colletotrichum lagenarium by MTT assay | 2006 | Journal of natural products, Dec, Volume: 69, Issue:12 | Bioactive oligostilbenoids from the stem bark of Hopea exalata. |
| AID667053 | Antifungal activity against Aspergillus niger at 50 ug/ml after 48 hrs by agar well diffusion method | 2012 | European journal of medicinal chemistry, Aug, Volume: 54 | Synthesis, antimicrobial and cytotoxic activities of sulfone linked bis heterocycles. |
| AID1247085 | Antifungal activity against Malassezia pachydermatis assessed as growth inhibition at 1 mg/well after 48 hrs by Well method | 2015 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19 | Synthesis of BF₃ catalyzed Mannich derivatives with excellent ee from phenylpropanolamine, study of their antimicrobial activity and molecular docking. |
| AID196663 | Antagonism of leuprolide-induced release of luteinizing hormone from rat pituitary cell | 1989 | Journal of medicinal chemistry, Sep, Volume: 32, Issue:9 | LH-RH antagonists: design and synthesis of a novel series of peptidomimetics. |
| AID491985 | Inhibition of human CYP11B1 expressed in hamster V79MZh cells | 2010 | Journal of medicinal chemistry, Jul-08, Volume: 53, Issue:13 | Isopropylidene substitution increases activity and selectivity of biphenylmethylene 4-pyridine type CYP17 inhibitors. |
| AID580179 | Antimicrobial activity against Candida albicans ATCC 10231 after 48 hrs by MTT assay | 2011 | Bioorganic & medicinal chemistry, Mar-01, Volume: 19, Issue:5 | Synthesis, structure, molecular docking, and structure-activity relationship analysis of enamines: 3-aryl-4-alkylaminofuran-2(5H)-ones as potential antibacterials. |
| AID659910 | Antifungal activity against Candida albicans NRRL Y-477 by two-fold serial dilution method | 2012 | European journal of medicinal chemistry, Jun, Volume: 52 | Design and synthesis of new 4-pyrazolin-3-yl-1,2,3-triazoles and 1,2,3-triazol-4-yl-pyrazolin-1-ylthiazoles as potential antimicrobial agents. |
| AID39704 | In vitro evaluation of minimum inhibitory concentration against Aspergillus fumigatus 33 | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20 | Synthesis and antifungal activity of new azole derivatives containing an N-acylmorpholine ring. |
| AID334242 | Antimicrobial activity against Escherichia coli NCTC 9002 after 24 hrs by microdilution technique | 2002 | Journal of natural products, Apr, Volume: 65, Issue:4 | Antimicrobial activities of a new schizozygane indoline alkaloid from Schizozygia coffaeoides and the revised structure of isoschizogaline. |
| AID491987 | Inhibition of CYP19 in human placental microsomes | 2010 | Journal of medicinal chemistry, Jul-08, Volume: 53, Issue:13 | Isopropylidene substitution increases activity and selectivity of biphenylmethylene 4-pyridine type CYP17 inhibitors. |
| AID572705 | Selectivity ratio, ratio of Kd for Mycobacterium smegmatis ATCC 700084 CYP164A2 to Kd for Mycobacterium avium CYP51 | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | Identification, characterization, and azole-binding properties of Mycobacterium smegmatis CYP164A2, a homolog of ML2088, the sole cytochrome P450 gene of Mycobacterium leprae. |
| AID641025 | Antifungal activity against Penicillium chrysogenum NCIM 738 after 48 hrs by agar well diffusion assay | 2012 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2 | Synthesis, characterization and in vitro biological evaluation of some novel diarylsulfonylureas as potential cytotoxic and antimicrobial agents. |
| AID26810 | Partition coefficient (logP) | 1985 | Journal of medicinal chemistry, Aug, Volume: 28, Issue:8 | Structural features of imidazole derivatives that enhance styrene oxide hydrolase activity in rat hepatic microsomes. |
| AID633952 | Antifungal activity against Aspergillus niger ATCC 6275 after 72 hrs by serial dilution technique | 2011 | Bioorganic & medicinal chemistry, Dec-15, Volume: 19, Issue:24 | Novel (E)-1-(4-methyl-2-(alkylamino)thiazol-5-yl)-3-arylprop-2-en-1-ones as potent antimicrobial agents. |
| AID1238923 | Antifungal activity against Candida parapsilosis ATCC 90018 WTBF-88 by microbroth dilution method | 2015 | Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17 | Synthesis and antifungal evaluation of head-to-head and head-to-tail bisamidine compounds. |
| AID492340 | Inhibition of CYP24A1 in human epidermal keratinocytes | 2010 | Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14 | Synthesis and CYP24A1 inhibitory activity of N-(2-(1H-imidazol-1-yl)-2-phenylethyl)arylamides. |
| AID405040 | Antifungal activity against Sporothrix schenckii P10012 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by Sensititre YeastOne method | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods. |
| AID588209 | Literature-mined public compounds from Greene et al multi-species hepatotoxicity modelling dataset | 2010 | Chemical research in toxicology, Jul-19, Volume: 23, Issue:7 | Developing structure-activity relationships for the prediction of hepatotoxicity. |
| AID644188 | Antifungal activity against Penicillium funiculosum ATCC 36839 treated for 72 hrs followed by sub-cultivated for 5 days by serial dilution method | 2012 | Bioorganic & medicinal chemistry, Feb-15, Volume: 20, Issue:4 | Synthesis of novel sulfonamide-1,2,4-triazoles, 1,3,4-thiadiazoles and 1,3,4-oxadiazoles, as potential antibacterial and antifungal agents. Biological evaluation and conformational analysis studies. |
| AID655584 | Antifungal activity against Candida tropicalis by microbroth dilution method | 2012 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8 | New triazole derivatives as antifungal agents: synthesis via click reaction, in vitro evaluation and molecular docking studies. |
| AID396955 | Antifungal activity against Aspergillus niger NCIM 596 at 100 ug/disk after 48 hrs by agar disc-diffusion method | 2009 | European journal of medicinal chemistry, May, Volume: 44, Issue:5 | Synthesis, antimicrobial and cytotoxic activities of 1,3,4-oxadiazoles, 1,3,4-thiadiazoles and 1,2,4-triazoles. |
| AID7232 | Inhibition of progesterone 6-beta-hydroxylase in rat hepatic microsomes | 1992 | Journal of medicinal chemistry, Jul-24, Volume: 35, Issue:15 | Stereoisomers of ketoconazole: preparation and biological activity. |
| AID549045 | Antifungal activity against Candida albicans CA2 after 48 hrs by broth microdilution method | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | In vitro activities of retigeric acid B alone and in combination with azole antifungal agents against Candida albicans. |
| AID49120 | Inhibitory activity against the Candida albicans (40 clinical isolates), determined at pH-5.8 | 1995 | Journal of medicinal chemistry, Oct-13, Volume: 38, Issue:21 | Antifungal agents. 9. 3-Aryl-4-[alpha-(1H-imidazol-1-yl)arylmethyl]pyrroles: a new class of potent anti-Candida agents. |
| AID1293498 | 1-octanol-potassium phosphate buffer distribution co-efficient, log D of the compound incubated overnight at pH 7.4 by shake-flask method | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5 | Thiazolino 2-Pyridone Amide Inhibitors of Chlamydia trachomatis Infectivity. |
| AID531180 | Antifungal activity against Trichophyton mentagrophytes ATCC MYA-4439 at 9.4 uM after 5 days by CLSI method | 2008 | Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7 | Potent in vitro antifungal activities of naturally occurring acetylenic acids. |
| AID1221956 | Apparent permeability from apical to basolateral side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2 | Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
| AID1160915 | Selectivity index, ratio of Ki for mouse CYP27B1 to Ki for human MBP-tagged CYP24A1 | 2014 | Journal of medicinal chemistry, Sep-25, Volume: 57, Issue:18 | Small-molecule inhibitors of 25-hydroxyvitamin D-24-hydroxylase (CYP24A1): synthesis and biological evaluation. |
| AID363716 | Antifungal activity against Microsporum gypseum C115 after 48 hrs by broth microdilution technique | 2008 | Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17 | In vitro antifungal activity of polyfunctionalized 2-(hetero)arylquinolines prepared through imino Diels-Alder reactions. |
| AID395647 | Antifungal activity against Candida albicans ATCC 10231 assessed as growth inhibition at 100 uM after 24 hrs | 2009 | European journal of medicinal chemistry, Jan, Volume: 44, Issue:1 | Penetratin and derivatives acting as antifungal agents. |
| AID586925 | Antileishmanial activity against wild type promastigotes of Leishmania major MHOM/JL/80/Friedlin assessed as inhibition of parasite growth after 72 hrs by MTT assay | 2011 | Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3 | Increased glycolytic ATP synthesis is associated with tafenoquine resistance in Leishmania major. |
| AID377673 | Antifungal activity against azole-resistant Candida albicans D10 after 48 hrs by NCCLS M27A method | 2006 | Journal of natural products, Jul, Volume: 69, Issue:7 | Phytochemistry and antifungal properties of the newly discovered tree Pleodendron costaricense. |
| AID405110 | Antimicrobial activity against Absidia sp. assessed as percent of susceptible isolates after 24 hrs | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | In vitro susceptibilities of 217 clinical isolates of zygomycetes to conventional and new antifungal agents. |
| AID596525 | Antifungal activity against Aspergillus flavus ATCC 9170 | 2011 | Bioorganic & medicinal chemistry, May-01, Volume: 19, Issue:9 | Antifungal, cytotoxic and SAR studies of a series of N-alkyl, N-aryl and N-alkylphenyl-1,4-pyrrolediones and related compounds. |
| AID530938 | Antifungal activity against Candida krusei ATCC 6258 at 9.4 uM after 48 hrs by CLSI method | 2008 | Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7 | Potent in vitro antifungal activities of naturally occurring acetylenic acids. |
| AID481665 | Antifungal activity against Candida zeylanoides NRRL Y-1774 after 24 hrs by broth microdilution assay | 2010 | European journal of medicinal chemistry, May, Volume: 45, Issue:5 | Synthesis and the selective antifungal activity of 5,6,7,8-tetrahydroimidazo[1,2-a]pyridine derivatives. |
| AID43008 | Inhibition of Candida tropicalis 156 growth for 24 hours in vitro. | 2001 | Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17 | 3-Phenyl-5-acyloxymethyl-2H,5H-furan-2-ones: synthesis and biological activity of a novel group of potential antifungal drugs. |
| AID633954 | Antifungal activity against Penicillium funiculosum ATCC 36839 after 72 hrs by serial dilution technique | 2011 | Bioorganic & medicinal chemistry, Dec-15, Volume: 19, Issue:24 | Novel (E)-1-(4-methyl-2-(alkylamino)thiazol-5-yl)-3-arylprop-2-en-1-ones as potent antimicrobial agents. |
| AID679463 | TP_TRANSPORTER: inhibition of Daunorubicin transport in G185 cells | 2002 | Antimicrobial agents and chemotherapy, Jan, Volume: 46, Issue:1 | Interaction of common azole antifungals with P glycoprotein. |
| AID160710 | Inhibitory activity against Prostaglandin G/H synthase (bovine seminal vesicles) | 1992 | Journal of medicinal chemistry, Aug-21, Volume: 35, Issue:17 | Novel 1-(pyridylphenyl)-1-phenyl-2-imidazolylethanols with topical antiinflammatory activity. |
| AID323057 | Antifungal activity against Candida albicans ATCC 10231 by micro-broth dilution method | 2008 | Bioorganic & medicinal chemistry, Jan-15, Volume: 16, Issue:2 | Antifungal and cytotoxic activities of some N-substituted aniline derivatives bearing a hetaryl fragment. |
| AID49262 | Percent resistance against Candida albicans (40 clinical isolates) at 256 micro g/mL (pH=5.8), activity is expressed as R%. | 1995 | Journal of medicinal chemistry, Oct-13, Volume: 38, Issue:21 | Antifungal agents. 9. 3-Aryl-4-[alpha-(1H-imidazol-1-yl)arylmethyl]pyrroles: a new class of potent anti-Candida agents. |
| AID1328452 | Inhibition of Cyp19 (unknown origin) | 2016 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 26, Issue:23 | Design, synthesis, and evaluation of (2S,4R)-Ketoconazole sulfonamide analogs as potential treatments for Metabolic Syndrome. |
| AID1079936 | Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source] | |||
| AID278214 | Increased sensitivity to growth inhibition in Saccharomyces cerevisiae KLN1 carrying erg1 pR269G allele after 24 hrs relative to wild type at 30 degC | 2007 | Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1 | Characterization of squalene epoxidase of Saccharomyces cerevisiae by applying terbinafine-sensitive variants. |
| AID426402 | Inhibition of recombinant CYP11B1 expressed in V79MZh11B1 cells at 0.2 uM | 2009 | European journal of medicinal chemistry, Jul, Volume: 44, Issue:7 | Novel CYP17 inhibitors: synthesis, biological evaluation, structure-activity relationships and modelling of methoxy- and hydroxy-substituted methyleneimidazolyl biphenyls. |
| AID1275145 | Antifungal activity against Candida krusei NRLL Y-7179 after 48 hrs by broth microdilution method | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Synthesis and biological evaluation of new naphthalene substituted thiosemicarbazone derivatives as potent antifungal and anticancer agents. |
| AID376048 | Antifungal activity against Epidermophyton floccosum C 114 by agar dilution method | 1999 | Journal of natural products, Oct, Volume: 62, Issue:10 | In vitro evaluation of antifungal properties of phenylpropanoids and related compounds acting against dermatophytes. |
| AID530930 | Antifungal activity against Fluconazole resistant Candida albicans isolate 17 at 9.4 uM after 48 hrs by CLSI method | 2008 | Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7 | Potent in vitro antifungal activities of naturally occurring acetylenic acids. |
| AID623359 | Antifungal activity against Candida albicans NRRL Y-12983 by NCCLS M27-A2 microbroth dilution method | 2011 | European journal of medicinal chemistry, Nov, Volume: 46, Issue:11 | Synthesis and anticandidal activity of new triazolothiadiazine derivatives. |
| AID221159 | Inhibition of lanosterol 14-alpha-demethylase in hamster hepatic microsomes | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | Selective inhibition of mammalian lanosterol 14 alpha-demethylase: a possible strategy for cholesterol lowering. |
| AID54927 | Inhibition of lauric acid hydroxylase cytochrome P450 4A | 1992 | Journal of medicinal chemistry, Jul-24, Volume: 35, Issue:15 | Stereoisomers of ketoconazole: preparation and biological activity. |
| AID32564 | In vitro minimum inhibitory concentration of compound was determined against Absidia corymbifera after 48 hr | 2000 | Bioorganic & medicinal chemistry letters, Aug-21, Volume: 10, Issue:16 | 3-Phenyl-5-methyl-2H,5H-furan-2-ones: tuning antifungal activity by varying substituents on the phenyl ring. |
| AID1557094 | Cytotoxicity against human HepG2 cells assessed as reduction in cell viability at 5 to 50 uM incubated for 24 hrs by XTT assay relative to control | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Antifungal activity, mode of action variability, and subcellular distribution of coumarin-based antifungal azoles. |
| AID1328449 | Inhibition of recombinant CYP17 (unknown origin) overexpressed in human AD293 cells using [21-3H]17alpha-hydroxyl-pregenolone as substrate preincubated for 60 mins followed by substrate addition measured after 4 hrs by Topcount method | 2016 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 26, Issue:23 | Design, synthesis, and evaluation of (2S,4R)-Ketoconazole sulfonamide analogs as potential treatments for Metabolic Syndrome. |
| AID262552 | Antifungal activity against Trichophyton rubrum | 2006 | Journal of medicinal chemistry, Apr-20, Volume: 49, Issue:8 | Structure-based optimization of azole antifungal agents by CoMFA, CoMSIA, and molecular docking. |
| AID1472623 | In vitro antifungal activity against Trichophyton rubrum after 7 days by serial dilution method | 2018 | Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1 | Novel Terminal Bipheny-Based Diapophytoene Desaturases (CrtN) Inhibitors as Anti-MRSA/VISR/LRSA Agents with Reduced hERG Activity. |
| AID774655 | Selectivity ratio of cytotoxic activity against mouse NIH/3T3 cells to antitrypanosomal activity against amastigote stage of Trypanosoma cruzi | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20 | Approaches to protozoan drug discovery: phenotypic screening. |
| AID330528 | Antifungal activity against Candida parapsilosis infected cyclophosphamide-immunocompromized Crl:CD1(ICR) mouse assessed as fungal density in kidney at 50 mg/kg, po for 5 days measured on day 12 | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Mar-13, Volume: 104, Issue:11 | High-throughput synergy screening identifies microbial metabolites as combination agents for the treatment of fungal infections. |
| AID596529 | Antifungal activity against Trichophyton mentagrophytes ATCC 9972 | 2011 | Bioorganic & medicinal chemistry, May-01, Volume: 19, Issue:9 | Antifungal, cytotoxic and SAR studies of a series of N-alkyl, N-aryl and N-alkylphenyl-1,4-pyrrolediones and related compounds. |
| AID53240 | Inhibition of rat Cytochrome P450 17A1 | 1998 | Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6 | Novel 17-azolyl steroids, potent inhibitors of human cytochrome 17 alpha-hydroxylase-C17,20-lyase (P450(17) alpha): potential agents for the treatment of prostate cancer. |
| AID530740 | Antifungal activity against Candida albicans ATCC 32354 at 9.4 uM after 48 hrs by CLSI method | 2008 | Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7 | Potent in vitro antifungal activities of naturally occurring acetylenic acids. |
| AID668005 | Inhibition of human CYP3A4 in liver microsomes | 2012 | Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9 | Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities. |
| AID481663 | Antifungal activity against Candida tropicalis NRRL Y-12968 after 24 hrs by broth microdilution assay | 2010 | European journal of medicinal chemistry, May, Volume: 45, Issue:5 | Synthesis and the selective antifungal activity of 5,6,7,8-tetrahydroimidazo[1,2-a]pyridine derivatives. |
| AID420074 | Antifungal activity against Candida parapsilosis after 24 hrs by broth microdilution assay | 2009 | Bioorganic & medicinal chemistry, Jun-01, Volume: 17, Issue:11 | Bulky 1,4-benzoxazine derivatives with antifungal activity. |
| AID486243 | Antifungal activity against Trichophyton mentagrophytes ATCC 9972 after 48 hrs | 2010 | European journal of medicinal chemistry, Jun, Volume: 45, Issue:6 | Naftifine-analogues as anti-Trypanosoma cruzi agents. |
| AID261013 | Inhibitory activity against Candida albicans | 2006 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 16, Issue:4 | Novel endoperoxides: synthesis and activity against Candida species. |
| AID48822 | In vitro Minimum lethal concentration was determined by microbroth dilution assay on Candida tropicalis | 1992 | Journal of medicinal chemistry, Jan, Volume: 35, Issue:1 | Synthesis, specificity, and antifungal activity of inhibitors of the Candida albicans delta 24-sterol methyltransferase. |
| AID313553 | Inhibition of hepatic CYP2C19 at 1 uM | 2008 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 18, Issue:1 | Synthesis, biological evaluation and molecular modelling studies of novel ACD- and ABD-ring steroidomimetics as inhibitors of CYP17. |
| AID1075572 | Antimicrobial activity against Fusarium solani NRRL 13414 after 48 to 72 hrs by microbroth dilution method | 2014 | European journal of medicinal chemistry, Mar-03, Volume: 74 | Synthesis and biological evaluation of thiazoline derivatives as new antimicrobial and anticancer agents. |
| AID39543 | In vitro antifungal activity against Aspergillus fumigatus | 1984 | Journal of medicinal chemistry, Jul, Volume: 27, Issue:7 | Antimycotic azoles. 7. Synthesis and antifungal properties of a series of novel triazol-3-ones. |
| AID294853 | Antifungal activity against Trichophyton rubrum after 7 days by microbroth dilution method | 2007 | European journal of medicinal chemistry, Sep, Volume: 42, Issue:9 | Synthesis of novel triazole derivatives as inhibitors of cytochrome P450 14alpha-demethylase (CYP51). |
| AID1233491 | Antimicrobial activity against Candida albicans MTCC 227 assessed as inhibition of visual microbial growth incubated for 48 to 72 hrs at 28 degC | 2015 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 25, Issue:14 | Thiophene and benzodioxole appended thiazolyl-pyrazoline compounds: Microwave assisted synthesis, antimicrobial and molecular docking studies. |
| AID150735 | High affinity constant at binding site of human P-Glycoprotein (P-gp) in two-affinity model | 2002 | Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26 | Pharmacophore model of drugs involved in P-glycoprotein multidrug resistance: explanation of structural variety (hypothesis). |
| AID214438 | In vitro minimum inhibitory concentration of compound was determined against Trichosporon beigelii after 24 hr r | 2000 | Bioorganic & medicinal chemistry letters, Aug-21, Volume: 10, Issue:16 | 3-Phenyl-5-methyl-2H,5H-furan-2-ones: tuning antifungal activity by varying substituents on the phenyl ring. |
| AID49259 | Tested for minimum subinhibitory concentration against Candida albicans 9 (Candida albicans) at pH 6.5. | 1994 | Journal of medicinal chemistry, Jun-24, Volume: 37, Issue:13 | Derivatives of a novel cyclopeptolide. 1. Synthesis, antifungal activity, and structure-activity relationships. |
| AID477745 | Antimicrobial activity against Trichophyton mentagrophytes after 24 hrs | 2010 | European journal of medicinal chemistry, Apr, Volume: 45, Issue:4 | An eco-friendly synthesis and antimicrobial activities of dihydro-2H-benzo- and naphtho-1,3-oxazine derivatives. |
| AID1104305 | Antifungal activity against plant isolate Aspergillus fumigatus at 28 degC measured after 72 hr by microdilution method | 2010 | Chemical & pharmaceutical bulletin, Feb, Volume: 58, Issue:2 | Sulfonamide-1,2,4-thiadiazole derivatives as antifungal and antibacterial agents: synthesis, biological evaluation, lipophilicity, and conformational studies. |
| AID362914 | Antifungal activity against Candida glabrata after 24 hrs by broth microdilution method | 2008 | Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17 | NO-donors. Part 17: Synthesis and antimicrobial activity of novel ketoconazole-NO-donor hybrid compounds. |
| AID47580 | Evaluation of In vitro antifungal activity against Candida albicans 2.01 by broth macro dilution method | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20 | Synthesis and antifungal activity of new azole derivatives containing an N-acylmorpholine ring. |
| AID537734 | Antifungal activity against yeast AD1-8u expressing Candida albicans CaMdr1p by agar disk diffusion assay | 2010 | European journal of medicinal chemistry, Nov, Volume: 45, Issue:11 | Analysis of physico-chemical properties of substrates of ABC and MFS multidrug transporters of pathogenic Candida albicans. |
| AID214835 | Antiproliferative activity against epimastigote form of Trypanosoma cruzi | 2002 | Journal of medicinal chemistry, Aug-29, Volume: 45, Issue:18 | Design, synthesis, and biological evaluation of aryloxyethyl thiocyanate derivatives against Trypanosoma cruzi. |
| AID386623 | Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells at 100 uM by confocal microscopy | 2008 | Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19 | Structural requirements for drug inhibition of the liver specific human organic cation transport protein 1. |
| AID262707 | Inhibition of human CYP11B1 expressed in V79 11B1 cells | 2006 | Journal of medicinal chemistry, Apr-06, Volume: 49, Issue:7 | Synthesis and evaluation of heteroaryl-substituted dihydronaphthalenes and indenes: potent and selective inhibitors of aldosterone synthase (CYP11B2) for the treatment of congestive heart failure and myocardial fibrosis. |
| AID322375 | Binding affinity to human His-tagged CYP51 expressed in Escherichia coli | 2008 | Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1 | Novel cholesterol biosynthesis inhibitors targeting human lanosterol 14alpha-demethylase (CYP51). |
| AID282734 | Inhibition of CYP26A1 in human MCF7 cells assessed as all-trans retinoic acid metabolism | 2005 | Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23 | Novel tetralone-derived retinoic acid metabolism blocking agents: synthesis and in vitro evaluation with liver microsomal and MCF-7 CYP26A1 cell assays. |
| AID295123 | Antifungal activity against Candida albicans ATCC 10231 at 20 ug after 72 hrs by disk diffusion method | 2007 | European journal of medicinal chemistry, Aug, Volume: 42, Issue:8 | Raman, FT-IR, NMR spectroscopic data and antimicrobial activity of bis[micro2-(benzimidazol-2-yl)-2-ethanethiolato-N,S,S-chloro-palladium(II)] dimer, [(micro2-CH2CH2NHNCC6H4)PdCl]2.C2H5OH complex. |
| AID323063 | Antifungal activity against Aspergillus niger ATCC 9029 by micro-broth dilution method | 2008 | Bioorganic & medicinal chemistry, Jan-15, Volume: 16, Issue:2 | Antifungal and cytotoxic activities of some N-substituted aniline derivatives bearing a hetaryl fragment. |
| AID568746 | Inhibition of CYP3A4 after 30 mins by fluorometric assay | 2011 | Journal of natural products, Jan-28, Volume: 74, Issue:1 | Cytochrome P450 3A4 inhibitory constituents of the wood of Taxus yunnanensis. |
| AID625283 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID420213 | Antimicrobial activity against Bacillus subtilis UFPEDA 16 after 20 hrs by twofold serial dilution technique | 2009 | European journal of medicinal chemistry, May, Volume: 44, Issue:5 | Synthesis, antimicrobial and cytotoxic activities of some 5-arylidene-4-thioxo-thiazolidine-2-ones. |
| AID575120 | Antifungal activity against Madurella mycetomatis isolate 83 by XTT assay | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Madurella mycetomatis is not susceptible to the echinocandin class of antifungal agents. |
| AID284099 | Antifungal activity against Candida neoformans ATCC 32264 after 48 hrs | 2007 | Bioorganic & medicinal chemistry, Jan-01, Volume: 15, Issue:1 | Synthesis and antifungal activity of (Z)-5-arylidenerhodanines. |
| AID102945 | Binding affinity at LH-RH receptor in rat pituitary using [125I]leuprolide as radioligand | 1989 | Journal of medicinal chemistry, Sep, Volume: 32, Issue:9 | LH-RH antagonists: design and synthesis of a novel series of peptidomimetics. |
| AID389811 | Inhibition of human CYP17 expressed in Escherichia coli | 2008 | Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24 | In vivo active aldosterone synthase inhibitors with improved selectivity: lead optimization providing a series of pyridine substituted 3,4-dihydro-1H-quinolin-2-one derivatives. |
| AID750212 | Antifungal activity against Saccharomyces cerevisiae assessed as diameter of inhibition zone at 0.5 mg/ml after 24 hrs by agar well diffusion method | 2013 | European journal of medicinal chemistry, Jun, Volume: 64 | Thiourea derivatives incorporating a hippuric acid moiety: synthesis and evaluation of antibacterial and antifungal activities. |
| AID1443992 | Total Cmax in human administered as single dose | 2014 | Hepatology (Baltimore, Md.), Sep, Volume: 60, Issue:3 | Human drug-induced liver injury severity is highly associated with dual inhibition of liver mitochondrial function and bile salt export pump. |
| AID1467479 | Antifungal activity against Aspergillus niger after 48 to 72 hrs by microdilution method | 2017 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 27, Issue:14 | Synthesis, SAR and molecular docking studies of benzo[d]thiazole-hydrazones as potential antibacterial and antifungal agents. |
| AID319757 | Antimicrobial activity against Fonsecaea compacta isolates | 2008 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 18, Issue:11 | Synthesis and SAR studies of biaryloxy-substituted triazoles as antifungal agents. |
| AID486240 | Antifungal activity against Aspergillus niger ATCC 9029 after 48 hrs | 2010 | European journal of medicinal chemistry, Jun, Volume: 45, Issue:6 | Naftifine-analogues as anti-Trypanosoma cruzi agents. |
| AID1130399 | Antifungal activity against Candida albicans B2630 infected in guinea pig cutaneous candidosis model at 2.5 mg/kg, po for 14 days measured on day 21 | 1979 | Journal of medicinal chemistry, Aug, Volume: 22, Issue:8 | Antimycotic imidazoles. part 4. Synthesis and antifungal activity of ketoconazole, a new potent orally active broad-spectrum antifungal agent. |
| AID406950 | Antifungal activity against Candida parapsilosis ATCC 22019 at 35 degC after 48 hrs by broth microdilution test | 2008 | Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13 | 1-[(3-Aryloxy-3-aryl)propyl]-1H-imidazoles, new imidazoles with potent activity against Candida albicans and dermatophytes. Synthesis, structure-activity relationship, and molecular modeling studies. |
| AID525139 | Antifungal activity against Fusarium moniliforme clade 1 by microdilution method | 2008 | Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6 | In vitro antifungal susceptibility and molecular characterization of clinical isolates of Fusarium verticillioides (F. moniliforme) and Fusarium thapsinum. |
| AID48257 | 90% inhibitory activity against the Candida. species (40 clinical isolates) was determined at pH-7.2 | 1995 | Journal of medicinal chemistry, Oct-13, Volume: 38, Issue:21 | Antifungal agents. 9. 3-Aryl-4-[alpha-(1H-imidazol-1-yl)arylmethyl]pyrroles: a new class of potent anti-Candida agents. |
| AID214270 | In vitro minimum inhibitory concentration of compound was determined against Trichophyton mentagrophytes after 120 hr | 2000 | Bioorganic & medicinal chemistry letters, Aug-21, Volume: 10, Issue:16 | 3-Phenyl-5-methyl-2H,5H-furan-2-ones: tuning antifungal activity by varying substituents on the phenyl ring. |
| AID1103205 | Antifungal activity against Fusarium graminearum isolate CE135 after 48 to 72 hr | 2004 | Journal of agricultural and food chemistry, Jun-02, Volume: 52, Issue:11 | Antifungal chalcones and new caffeic acid esters from Zuccagnia punctata acting against soybean infecting fungi. |
| AID1157295 | Antifungal activity against Aspergillus fumigatus 07544 assessed as growth inhibition by automatic microplate reader analysis | 2014 | Journal of natural products, May-23, Volume: 77, Issue:5 | Polyhydroxy cyclohexanols from a Dendrodochium sp. fungus associated with the sea cucumber Holothuria nobilis Selenka. |
| AID632565 | Antifungal activity against Candida albicans at 200 ug/mL after 48 hrs by agar cup diffusion assay | 2011 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 21, Issue:24 | A new antifungal briarane diterpenoid from the gorgonian Junceella juncea Pallas. |
| AID549049 | Antifungal activity against Candida albicans CA132 after 48 hrs by broth microdilution method | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | In vitro activities of retigeric acid B alone and in combination with azole antifungal agents against Candida albicans. |
| AID425724 | Cytotoxicity against HBMEC assessed as LDH release at 10 ug/mL | 2007 | Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12 | Effect of antimicrobial compounds on Balamuthia mandrillaris encystment and human brain microvascular endothelial cell cytopathogenicity. |
| AID1156979 | Inhibition of human recombinant CYP3A4 at 10 uM preincubated for 10 mins followed by NADPH addition measured after 30 mins by luciferase reporter gene assay | 2014 | European journal of medicinal chemistry, Aug-18, Volume: 83 | Aryl-1,3,5-triazine derivatives as histamine H4 receptor ligands. |
| AID48943 | Tested for minimum inhibitory concentration against Candida albicans 4 (Candida albicans) at pH 6.5. | 1994 | Journal of medicinal chemistry, Jun-24, Volume: 37, Issue:13 | Derivatives of a novel cyclopeptolide. 1. Synthesis, antifungal activity, and structure-activity relationships. |
| AID37717 | In vitro evaluation of minimum inhibitory concentration against Aspergillus niger 18 | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20 | Synthesis and antifungal activity of new azole derivatives containing an N-acylmorpholine ring. |
| AID211472 | Evaluation of In vitro antifungal activity against Torulopsis glabrata 78 by broth macro dilution method | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20 | Synthesis and antifungal activity of new azole derivatives containing an N-acylmorpholine ring. |
| AID48638 | Evaluation of In vitro antifungal activity against Candida tropicalis 2.11 by broth macro dilution method | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20 | Synthesis and antifungal activity of new azole derivatives containing an N-acylmorpholine ring. |
| AID340950 | Antifungal activity against Candida albicans isolates from HIV infected patient during fluconazole therapy by NCCLS M27-A2 method | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8 | Cross-resistance to medical and agricultural azole drugs in yeasts from the oropharynx of human immunodeficiency virus patients and from environmental Bavarian vine grapes. |
| AID717025 | Antifungal activity against Candida utilis NRRL Y-900 after 24 hrs by microdilution susceptibility assay | 2012 | European journal of medicinal chemistry, Dec, Volume: 58 | Synthesis and biological evaluation of some hydrazone derivatives as new anticandidal and anticancer agents. |
| AID49631 | Minimum inhibitory concentration of compound for antifungal activity against Candida albicans 1 | 2000 | Bioorganic & medicinal chemistry letters, Oct-02, Volume: 10, Issue:19 | Novel antifungals based on 4-substituted imidazole: a combinatorial chemistry approach to lead discovery and optimization. |
| AID45325 | Evaluation of In vitro antifungal activity against Candida albicans 31 by broth macro dilution method | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20 | Synthesis and antifungal activity of new azole derivatives containing an N-acylmorpholine ring. |
| AID1171982 | Antibacterial activity against Staphylococcus aureus MTCC 96 assessed as zone of inhibition at 1 mg/disc after 24 hrs by disc diffusion method | 2015 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2 | Facile and diastereoselective synthesis of 3,2'-spiropyrrolidine-oxindoles derivatives, their molecular docking and antiproliferative activities. |
| AID664303 | Antifungal activity against Candida albicans MTCC 183 at 100 ug/disc by paper disc diffusion technique | 2012 | European journal of medicinal chemistry, Jul, Volume: 53 | Synthesis of benzimidazolyl-1,3,4-oxadiazol-2ylthio-N-phenyl (benzothiazolyl) acetamides as antibacterial, antifungal and antituberculosis agents. |
| AID395379 | Antifungal activity against Hanseniaspora guilliermondii DSM 3432 at 1 ug after 72 hrs by disk diffusion method | 2009 | European journal of medicinal chemistry, Jan, Volume: 44, Issue:1 | Synthesis, Raman, FT-IR, NMR spectroscopic data and antimicrobial activity of mixed aza-oxo-thia macrocyclic compounds. |
| AID771362 | Growth inhibition of human MCF7 cells at 50 uM after 48 hrs by SRB assay relative to control | 2013 | European journal of medicinal chemistry, Oct, Volume: 68 | Cytotoxic effect of novel dehydroepiandrosterone derivatives on different cancer cell lines. |
| AID463410 | Antimicrobial activity against Trichoderma viride at 1000 ug after 72 hrs by cup plate method | 2010 | European journal of medicinal chemistry, Mar, Volume: 45, Issue:3 | Antimicrobial study of newly synthesized 6-substituted indolo[1,2-c]quinazolines. |
| AID49117 | Tested In vitro for antifungal activity at pH 5.8 | 2002 | Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13 | Antifungal agents. 10. New derivatives of 1-[(aryl)[4-aryl-1H-pyrrol-3-yl]methyl]-1H-imidazole, synthesis, anti-candida activity, and quantitative structure-analysis relationship studies. |
| AID359384 | Antifungal activity against Candida albicans 44506 in Sabouraud dextrose broth after 18 to 24 hrs by twofold broth dilution method | 1992 | Journal of natural products, Nov, Volume: 55, Issue:11 | Antifungal activity of meridine, a natural product from the marine sponge Corticium sp. |
| AID452180 | Inhibition of Yarrowia lipolytica 24-SMT assessed as ergosterol-3-trimethylsilyl derivative level at 0.2 ug/mL after 48 hrs by GC-MS analysis relative to untreated control | 2009 | Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23 | Side chain azasteroids and thiasteroids as sterol methyltransferase inhibitors in ergosterol biosynthesis. |
| AID362811 | Antifungal activity against Curvularia lunata at 200 ug after 48 hrs by agar disc-diffusion method | 2008 | European journal of medicinal chemistry, May, Volume: 43, Issue:5 | Synthesis and antimicrobial activity of novel sulfone-linked bis heterocycles. |
| AID363958 | Antimicrobial activity against Cryptococcus neoformans IM 031631 isolate at 6.25 ug/ml after 48 hrs | 2008 | Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17 | In vitro antifungal activity of polyfunctionalized 2-(hetero)arylquinolines prepared through imino Diels-Alder reactions. |
| AID1456577 | Antifungal activity against Candida albicans isolate SC5314 by micro-broth dilution method | 2017 | Bioorganic & medicinal chemistry letters, 05-15, Volume: 27, Issue:10 | Design, synthesis, and in vitro evaluation of novel antifungal triazoles. |
| AID463417 | Antimicrobial activity against Aspergillus niger after 24 hrs by liquid dilution method | 2010 | European journal of medicinal chemistry, Mar, Volume: 45, Issue:3 | Antimicrobial study of newly synthesized 6-substituted indolo[1,2-c]quinazolines. |
| AID363738 | Antimicrobial activity against Candida albicans C128 isolate at 6.25 ug/ml after 24 hrs | 2008 | Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17 | In vitro antifungal activity of polyfunctionalized 2-(hetero)arylquinolines prepared through imino Diels-Alder reactions. |
| AID426398 | Inhibition of human CYP17 expressed in Escherichia coli coexpressing NADPH-P450 reductase | 2009 | European journal of medicinal chemistry, Jul, Volume: 44, Issue:7 | Novel CYP17 inhibitors: synthesis, biological evaluation, structure-activity relationships and modelling of methoxy- and hydroxy-substituted methyleneimidazolyl biphenyls. |
| AID241487 | In vitro inhibitory concentration against Cytochrome P450 17 expressed in Escherichia coli | 2005 | Journal of medicinal chemistry, Apr-21, Volume: 48, Issue:8 | Novel C-17-heteroaryl steroidal CYP17 inhibitors/antiandrogens: synthesis, in vitro biological activity, pharmacokinetics, and antitumor activity in the LAPC4 human prostate cancer xenograft model. |
| AID533803 | Antifungal activity against Rhizopus CL35 by agar dilution method | 2010 | European journal of medicinal chemistry, Nov, Volume: 45, Issue:11 | Synthesis and biological evaluation of N-antipyrine-4-substituted amino-3-chloromaleimide derivatives. |
| AID590621 | Antifungal activity against Fusarium solani assessed as zone of inhibition at 200 ug/ml after 48 hrs by disc diffusion method | 2011 | European journal of medicinal chemistry, Apr, Volume: 46, Issue:4 | Synthesis and biological activity of 2-(bis((1,3,4-oxadiazolyl/1,3,4-thiadiazolyl)methylthio)methylene)malononitriles. |
| AID402936 | Inhibition of human CYP3A4 by radiometric assay | 2004 | Journal of natural products, Jul, Volume: 67, Issue:7 | Sesquiterpenes and flavonol glycosides from Zingiber aromaticum and their CYP3A4 and CYP2D6 inhibitory activities. |
| AID302122 | Antifungal activity against fluconazole-resistant Candida albicans 0511655 after 24 hrs | 2007 | Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22 | Synthesis and antifungal activities of novel 2-aminotetralin derivatives. |
| AID623357 | Antifungal activity against Candida krusei NRRL Y-7179 by NCCLS M27-A2 microbroth dilution method | 2011 | European journal of medicinal chemistry, Nov, Volume: 46, Issue:11 | Synthesis and anticandidal activity of new triazolothiadiazine derivatives. |
| AID1449628 | Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-taurocholate transport into vesicles incubated for 5 mins by Topcount based rapid filtration method | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12 | Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification. |
| AID83858 | Effect on total serum cholesterol in male hamsters at a dose of 100 mg/kg orally administered for 14 days | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | Selective inhibition of mammalian lanosterol 14 alpha-demethylase: a possible strategy for cholesterol lowering. |
| AID48941 | Tested for minimum inhibitory concentration against Candida albicans 3 (Candida albicans) at pH 6.5. | 1994 | Journal of medicinal chemistry, Jun-24, Volume: 37, Issue:13 | Derivatives of a novel cyclopeptolide. 1. Synthesis, antifungal activity, and structure-activity relationships. |
| AID717022 | Antifungal activity against Candida albicans clinical isolate after 24 hrs by microdilution susceptibility assay | 2012 | European journal of medicinal chemistry, Dec, Volume: 58 | Synthesis and biological evaluation of some hydrazone derivatives as new anticandidal and anticancer agents. |
| AID1223622 | Inhibition of CYP3A4 activity in human liver microsomes using midazolam as a substrate by LC/MS analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4 | Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID679459 | TP_TRANSPORTER: transepithelial transport (basal to apical) in Caco-2 cells | 1998 | European journal of pharmacology, Oct-09, Volume: 358, Issue:3 | Interaction with P-glycoprotein and transport of erythromycin, midazolam and ketoconazole in Caco-2 cells. |
| AID611680 | Antifungal activity against Septoria tritici at 0.05 mg by agar diffusion method | 2011 | Journal of natural products, Jul-22, Volume: 74, Issue:7 | Bioactive 11,20-epoxy-3,5(16)-diene briarane diterpenoids from the South China Sea gorgonian Dichotella gemmacea. |
| AID207138 | Ability to inhibit the Steroid 17-alpha-hydroxylase/17,20 lyase enzyme by 50%. | 1995 | Journal of medicinal chemistry, Jun-23, Volume: 38, Issue:13 | Novel steroidal inhibitors of human cytochrome P45017 alpha (17 alpha-hydroxylase-C17,20-lyase): potential agents for the treatment of prostatic cancer. |
| AID590625 | Antifungal activity against Aspergillus niger assessed as zone of inhibition at 200 ug/ml after 48 hrs by disc diffusion method | 2011 | European journal of medicinal chemistry, Apr, Volume: 46, Issue:4 | Synthesis and biological activity of 2-(bis((1,3,4-oxadiazolyl/1,3,4-thiadiazolyl)methylthio)methylene)malononitriles. |
| AID645286 | Antifungal activity against Saccharomyces cerevisiae at 50 ug/ml after 48 hrs by agar well diffusion method | 2012 | European journal of medicinal chemistry, Apr, Volume: 50 | Regioselective synthesis and antimicrobial activities of some novel aryloxyacetic acid derivatives. |
| AID1275146 | Antifungal activity against Candida zeylanoides NRLL Y-1774 after 48 hrs by broth microdilution method | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Synthesis and biological evaluation of new naphthalene substituted thiosemicarbazone derivatives as potent antifungal and anticancer agents. |
| AID1443995 | Hepatotoxicity in human assessed as drug-induced liver injury | 2014 | Hepatology (Baltimore, Md.), Sep, Volume: 60, Issue:3 | Human drug-induced liver injury severity is highly associated with dual inhibition of liver mitochondrial function and bile salt export pump. |
| AID125939 | In vitro antifungal activity against Microsporum canis ATCC 44459 | 1988 | Journal of medicinal chemistry, Oct, Volume: 31, Issue:10 | Studies on antifungal agents. 23. Novel substituted 3,5-diphenyl-3-(1H-imidazol-1-ylmethyl)- 2-alkylisoxazolidine derivatives. |
| AID260491 | Opening large conductance calcium-activated potassium channel in bovine smooth muscle cells at 100 uM | 2006 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 16, Issue:4 | Partial structures of ketoconazole as modulators of the large conductance calcium-activated potassium channel (BK(Ca)). |
| AID1324374 | Antifungal activity against Penicillium notatum by agar streak dilution method | 2016 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 26, Issue:22 | Novel substituted hydrazono indolo[2,1-b]quinazoline-6,12-dione analogues as cytostatic agents: Synthesis, crystal structure, biological evaluation and molecular docking studies. |
| AID417960 | Antifungal activity against Candida tropicalis after 48 hrs by broth microdilution technique | 2009 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6 | Relation between lipophilicity of alkyl gallates and antifungal activity against yeasts and filamentous fungi. |
| AID588220 | Literature-mined public compounds from Kruhlak et al phospholipidosis modelling dataset | 2008 | Toxicology mechanisms and methods, , Volume: 18, Issue:2-3 | Development of a phospholipidosis database and predictive quantitative structure-activity relationship (QSAR) models. |
| AID395376 | Antifungal activity against Candida albicans ATCC 10231 at 1 ug after 72 hrs by disk diffusion method | 2009 | European journal of medicinal chemistry, Jan, Volume: 44, Issue:1 | Synthesis, Raman, FT-IR, NMR spectroscopic data and antimicrobial activity of mixed aza-oxo-thia macrocyclic compounds. |
| AID1495446 | Inhibition of CYP3A4 (unknown origin) by CYP3A4 P450-Glo assay | |||
| AID1199393 | Inhibition of human CYP17 using 17alpha-hydroxypregnenolone substrate | 2015 | Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5 | Discovery and development of Galeterone (TOK-001 or VN/124-1) for the treatment of all stages of prostate cancer. |
| AID48821 | The compound was tested for antifungal activity against Candida tropicalis MY1012 using agar dilution assay | 1987 | Journal of medicinal chemistry, Aug, Volume: 30, Issue:8 | Lysosomotropic agents. 7. Broad-spectrum antifungal activity of lysosomotropic detergents. |
| AID340958 | Antifungal activity against Candida norvegensis isolates from grapes by NCCLS M27-A2 method | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8 | Cross-resistance to medical and agricultural azole drugs in yeasts from the oropharynx of human immunodeficiency virus patients and from environmental Bavarian vine grapes. |
| AID1557074 | Antifungal activity against ERG11/ERG3 knocked out Candida albicans SN152 assessed as zone of inhibition at 25 ug incubated for 48 hrs by disk diffusion method | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Antifungal activity, mode of action variability, and subcellular distribution of coumarin-based antifungal azoles. |
| AID623355 | Antifungal activity against Candida glabrata clinical isolate (Osmangazi university) by NCCLS M27-A2 microbroth dilution method | 2011 | European journal of medicinal chemistry, Nov, Volume: 46, Issue:11 | Synthesis and anticandidal activity of new triazolothiadiazine derivatives. |
| AID86930 | Percentage lowering of the total serum cholesterol in male hamsters at a dose of 100 mg/dL orally administered for 14 days | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | Selective inhibition of mammalian lanosterol 14 alpha-demethylase: a possible strategy for cholesterol lowering. |
| AID1177650 | Inhibition of human aldosterone synthase expressed in yeast cells | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12 | Aldosterone synthase inhibitors as promising treatments for mineralocorticoid dependent cardiovascular and renal diseases. |
| AID378128 | Inhibition of human liver microsome CYP3A4 in assessed as [14C]formaldehyde formation | 2005 | Journal of natural products, Jan, Volume: 68, Issue:1 | Potent CYP3A4 inhibitory constituents of Piper cubeba. |
| AID494181 | Antimicrobial activity against Candida albicans by broth microdilution method | 2010 | European journal of medicinal chemistry, Aug, Volume: 45, Issue:8 | Antimicrobial activity and a SAR study of some novel benzimidazole derivatives bearing hydrazone moiety. |
| AID131263 | Tested for efficacy of compound in experimental vaginal candidosis (mouse) after oral treatment at dosage of 4 x150 mg kg e-1 | 1994 | Journal of medicinal chemistry, Jun-24, Volume: 37, Issue:13 | Derivatives of a novel cyclopeptolide. 1. Synthesis, antifungal activity, and structure-activity relationships. |
| AID480595 | Inhibition of human recombinant CYP3A4 | 2010 | Journal of medicinal chemistry, May-27, Volume: 53, Issue:10 | Second generation analogues of the cancer drug clinical candidate tipifarnib for anti-Chagas disease drug discovery. |
| AID1435411 | Anti-fungal activity against Candida albicans ATCC 10231 measured after 24 hrs by microtiter broth dilution method | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Design, synthesis and antimicrobial evaluation of novel benzoxazole derivatives. |
| AID287383 | Antifungal activity against Hanseniaspora guilliermondii after 24 hrs by disk diffusion method | 2007 | European journal of medicinal chemistry, Feb, Volume: 42, Issue:2 | Synthesis, characterization and antimicrobial activity of Fe(II), Zn(II), Cd(II) and Hg(II) complexes with 2,6-bis(benzimidazol-2-yl) pyridine ligand. |
| AID39696 | In vitro antifungal activity against Aspergillus fumigatus ATCC 28212 | 1988 | Journal of medicinal chemistry, Oct, Volume: 31, Issue:10 | Studies on antifungal agents. 23. Novel substituted 3,5-diphenyl-3-(1H-imidazol-1-ylmethyl)- 2-alkylisoxazolidine derivatives. |
| AID1196733 | Antifungal activity against Candida glabrata clinical isolate after 48 hrs by broth microdilution assay | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | A novel series of thiazolyl-pyrazoline derivatives: synthesis and evaluation of antifungal activity, cytotoxicity and genotoxicity. |
| AID262706 | Inhibition of human CYP11B2 expressed in Schizosaccharomyces pombe at 500 nM | 2006 | Journal of medicinal chemistry, Apr-06, Volume: 49, Issue:7 | Synthesis and evaluation of heteroaryl-substituted dihydronaphthalenes and indenes: potent and selective inhibitors of aldosterone synthase (CYP11B2) for the treatment of congestive heart failure and myocardial fibrosis. |
| AID448515 | Antimicrobial activity against Alternaria alternata at 30 ug/mL after 16 to 20 hrs by disk diffusion method | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11 | Synthesis of some novel pyrazolo[3,4-b]pyridine and pyrazolo[3,4-d]pyrimidine derivatives bearing 5,6-diphenyl-1,2,4-triazine moiety as potential antimicrobial agents. |
| AID1130377 | Antifungal activity against Cryptococcus neoformans assessed as growth inhibition in sabouraud broth after 14 days | 1979 | Journal of medicinal chemistry, Aug, Volume: 22, Issue:8 | Antimycotic imidazoles. part 4. Synthesis and antifungal activity of ketoconazole, a new potent orally active broad-spectrum antifungal agent. |
| AID395649 | Antifungal activity against Candida albicans ATCC 10231 assessed as growth inhibition at 25 uM after 24 hrs | 2009 | European journal of medicinal chemistry, Jan, Volume: 44, Issue:1 | Penetratin and derivatives acting as antifungal agents. |
| AID407006 | Antimicrobial activity against Candida albicans FH1 dissociated biofilms at cell density of 10'8 cells/ml after 48 hrs by XTT assay | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | Role for cell density in antifungal drug resistance in Candida albicans biofilms. |
| AID405092 | Antimicrobial activity against Rhizopus sp. after 24 hrs | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | In vitro susceptibilities of 217 clinical isolates of zygomycetes to conventional and new antifungal agents. |
| AID723701 | Antifungal activity against Aspergillus niger ATCC 6275 after 72 hrs by serial dilution technique | 2013 | Bioorganic & medicinal chemistry, Jan-15, Volume: 21, Issue:2 | Synthesis and biological evaluation of some 5-arylidene-2-(1,3-thiazol-2-ylimino)-1,3-thiazolidin-4-ones as dual anti-inflammatory/antimicrobial agents. |
| AID486235 | Antifungal activity against Candida tropicalis C 131 2000 after 48 hrs | 2010 | European journal of medicinal chemistry, Jun, Volume: 45, Issue:6 | Naftifine-analogues as anti-Trypanosoma cruzi agents. |
| AID53375 | Inhibition of 17-alpha-hydroxylase enzyme, cytochrome P450 17A1 of human testicular microsomes | 1996 | Journal of medicinal chemistry, Aug-16, Volume: 39, Issue:17 | 3- and 4-pyridylalkyl adamantanecarboxylates: inhibitors of human cytochrome P450(17 alpha) (17 alpha-hydroxylase/C17,20-lyase). Potential nonsteroidal agents for the treatment of prostatic cancer. |
| AID1443991 | Induction of mitochondrial dysfunction in Sprague-Dawley rat liver mitochondria assessed as inhibition of mitochondrial respiration per mg mitochondrial protein measured for 20 mins by A65N-1 oxygen probe based fluorescence assay | 2014 | Hepatology (Baltimore, Md.), Sep, Volume: 60, Issue:3 | Human drug-induced liver injury severity is highly associated with dual inhibition of liver mitochondrial function and bile salt export pump. |
| AID208220 | Inhibition of Trichosporon beigelli 1188 for 48 hours in vitro. | 2001 | Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17 | 3-Phenyl-5-acyloxymethyl-2H,5H-furan-2-ones: synthesis and biological activity of a novel group of potential antifungal drugs. |
| AID511038 | Antimicrobial activity against Fusarium solani NCIM 1330 at 100 ug/disk after 48 hrs by agar disc-diffusion method | 2010 | European journal of medicinal chemistry, Sep, Volume: 45, Issue:9 | Synthesis and bioassay of aminosulfonyl-1,3,4-oxadiazoles and their interconversion to 1,3,4-thiadiazoles. |
| AID530949 | Antifungal activity against Candida tropicalis ATCC 750 at 9.4 uM after 48 hrs by CLSI method | 2008 | Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7 | Potent in vitro antifungal activities of naturally occurring acetylenic acids. |
| AID1130393 | Antifungal activity against Candida albicans B2630 infected in ovariectomized and hysterectomized Wistar rat vaginal candidosis model at 1.25 mg/kg, po for 14 days by prophylactic treatment | 1979 | Journal of medicinal chemistry, Aug, Volume: 22, Issue:8 | Antimycotic imidazoles. part 4. Synthesis and antifungal activity of ketoconazole, a new potent orally active broad-spectrum antifungal agent. |
| AID1171993 | Antibacterial activity against Staphylococcus aureus MTCC 96 assessed as inhibition of visual growth after 24 hrs | 2015 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2 | Facile and diastereoselective synthesis of 3,2'-spiropyrrolidine-oxindoles derivatives, their molecular docking and antiproliferative activities. |
| AID348961 | Antifungal activity against Candida albicans after 48 hrs by MTT assay | 2008 | European journal of medicinal chemistry, Jul, Volume: 43, Issue:7 | Synthesis and antimicrobial activities of 7-O-modified genistein derivatives. |
| AID1442001 | Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of ASP+ after 2 mins by fluorescence assay | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Discovery of Competitive and Noncompetitive Ligands of the Organic Cation Transporter 1 (OCT1; SLC22A1). |
| AID633915 | Antifungal activity against Candida albicans PYCC 3436 by twofold serial dilution technique | 2012 | European journal of medicinal chemistry, Jan, Volume: 47, Issue:1 | Isoxazoles incorporated N-substituted decahydroquinolines: a precursor to the next generation antimicrobial drug. |
| AID1221962 | Efflux ratio of permeability from apical to basolateral side over basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY335979 | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2 | Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
| AID242448 | Displacement of [3H]R-1881 from Androgen receptor of PC3-AR cells; - = not determined | 2005 | Journal of medicinal chemistry, Apr-21, Volume: 48, Issue:8 | Novel C-17-heteroaryl steroidal CYP17 inhibitors/antiandrogens: synthesis, in vitro biological activity, pharmacokinetics, and antitumor activity in the LAPC4 human prostate cancer xenograft model. |
| AID405067 | Antifungal activity against Candida krusei ATCC 6258 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by Sensititre YeastOne method | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods. |
| AID1181468 | Inhibition of recombinant human CYP3A4 preincubated at 10 uM for 5 mins before fluorescent substrate addition by fluorescence assay | 2014 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 24, Issue:15 | Synthesis and biological evaluation of 3-phenethylazetidine derivatives as triple reuptake inhibitors. |
| AID255081 | Inhibitory concentration against human cytochrome P450 11B2 expressed in fission yeast, incubated with [14C]deoxycorticosterone | 2005 | Journal of medicinal chemistry, Oct-20, Volume: 48, Issue:21 | Heteroaryl-substituted naphthalenes and structurally modified derivatives: selective inhibitors of CYP11B2 for the treatment of congestive heart failure and myocardial fibrosis. |
| AID635006 | Antifungal activity against Curvularia lunata NCIM 716 assessed as zone of inhibition at 100 ug/disc after 48 hrs by disk diffusion method | 2012 | European journal of medicinal chemistry, Jan, Volume: 47, Issue:1 | Synthesis, antimicrobial, antimycobacterial and structure-activity relationship of substituted pyrazolo-, isoxazolo-, pyrimido- and mercaptopyrimidocyclohepta[b]indoles. |
| AID406858 | Antimicrobial activity against Candida albicans SC5314 dissociated biofilms at cell density of 10'3 cells/ml after 48 hrs by XTT assay | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | Role for cell density in antifungal drug resistance in Candida albicans biofilms. |
| AID295129 | Antifungal activity against Hanseniaspora guilliermondii DSM 3432 at 20 ug after 72 hrs by disk diffusion method | 2007 | European journal of medicinal chemistry, Aug, Volume: 42, Issue:8 | Raman, FT-IR, NMR spectroscopic data and antimicrobial activity of bis[micro2-(benzimidazol-2-yl)-2-ethanethiolato-N,S,S-chloro-palladium(II)] dimer, [(micro2-CH2CH2NHNCC6H4)PdCl]2.C2H5OH complex. |
| AID102944 | Apparent receptor density at 3.16*10e-6 M concentration | 1989 | Journal of medicinal chemistry, Sep, Volume: 32, Issue:9 | LH-RH antagonists: design and synthesis of a novel series of peptidomimetics. |
| AID525142 | Antifungal activity against Fusarium thapsinum by microdilution method | 2008 | Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6 | In vitro antifungal susceptibility and molecular characterization of clinical isolates of Fusarium verticillioides (F. moniliforme) and Fusarium thapsinum. |
| AID363733 | Antimicrobial activity against Candida albicans C127 isolate at 6.25 ug/ml after 24 hrs | 2008 | Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17 | In vitro antifungal activity of polyfunctionalized 2-(hetero)arylquinolines prepared through imino Diels-Alder reactions. |
| AID362808 | Antifungal activity against Fusarium solani at 100 ug after 48 hrs by agar disc-diffusion method | 2008 | European journal of medicinal chemistry, May, Volume: 43, Issue:5 | Synthesis and antimicrobial activity of novel sulfone-linked bis heterocycles. |
| AID287714 | Antitrypanosomatid activity against Trypanosoma cruzi CL Brener epimastigotes assessed as reduction of growth after 5 days | 2007 | Bioorganic & medicinal chemistry, Apr-01, Volume: 15, Issue:7 | Second generation of 5-ethenylbenzofuroxan derivatives as inhibitors of Trypanosoma cruzi growth: synthesis, biological evaluation, and structure-activity relationships. |
| AID429269 | Antifungal activity against Aspergillus niger at 1000 ug/ml after 72 hrs by agar diffusion method | 2009 | European journal of medicinal chemistry, Aug, Volume: 44, Issue:8 | Mono and bis-6-arylbenzimidazo[1,2-c]quinazolines: a new class of antimicrobial agents. |
| AID1103206 | Antifungal activity against Fusarium graminearum isolate CE170 after 48 to 72 hr | 2004 | Journal of agricultural and food chemistry, Jun-02, Volume: 52, Issue:11 | Antifungal chalcones and new caffeic acid esters from Zuccagnia punctata acting against soybean infecting fungi. |
| AID290147 | Antibacterial activity against Staphylococcus aureus after 24 hrs by MTT colorimetric method | 2007 | European journal of medicinal chemistry, Apr, Volume: 42, Issue:4 | Synthesis and antimicrobial activities of Schiff bases derived from 5-chloro-salicylaldehyde. |
| AID632001 | Toxicity in CBA mouse infected with Leishmania amazonensis MHOM/ BR/77/LTB0016 assessed as change in leukocytes count at 50 mg/kg, po qd for 30 days administered 4 week post infection measured up to week 21 | 2011 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 21, Issue:24 | Synthesis and antileishmanial evaluation of 1-aryl-4-(4,5-dihydro-1H-imidazol-2-yl)-1H-pyrazole derivatives. |
| AID1456579 | Antifungal activity against Cryptococcus neoformans isolate 32605 by micro-broth dilution method | 2017 | Bioorganic & medicinal chemistry letters, 05-15, Volume: 27, Issue:10 | Design, synthesis, and in vitro evaluation of novel antifungal triazoles. |
| AID361270 | Binding affinity to recombinant CYP3A4 expressed in Escherichia coli assessed as spectral dissociation constant by spectrophotometric equilibrium binding titration method | 2007 | The Journal of biological chemistry, Mar-02, Volume: 282, Issue:9 | Multiple sequential steps involved in the binding of inhibitors to cytochrome P450 3A4. |
| AID635004 | Antifungal activity against Fusarium solani NCIM 1330 assessed as zone of inhibition at 100 ug/disc after 48 hrs by disk diffusion method | 2012 | European journal of medicinal chemistry, Jan, Volume: 47, Issue:1 | Synthesis, antimicrobial, antimycobacterial and structure-activity relationship of substituted pyrazolo-, isoxazolo-, pyrimido- and mercaptopyrimidocyclohepta[b]indoles. |
| AID473745 | Inhibition of human recombinant CYP3A4 assessed as biotransformation of 7-hydroxyquinoline to 7-benzyloxyquinoline measured every minute for 15 mins by fluorescence intensity assay | 2010 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 20, Issue:7 | Potent and selective inhibition of human cytochrome P450 3A4 by seco-pancratistatin structural analogs. |
| AID1300879 | Antifungal activity against Candida glabrata clinical isolate after 24 hrs by broth microdilution method | 2016 | European journal of medicinal chemistry, Jul-19, Volume: 117 | Novel 1,3-thiazolidin-4-one derivatives as promising anti-Candida agents endowed with anti-oxidant and chelating properties. |
| AID1055307 | Antifungal activity against Candida tropicalis ATCC 13803 at 50 ug after 72 hrs by disk diffusion method | 2013 | European journal of medicinal chemistry, , Volume: 70 | Phosphorus-nitrogen compounds part 27. Syntheses, structural characterizations, antimicrobial and cytotoxic activities, and DNA interactions of new phosphazenes bearing secondary amino and pendant (4-fluorobenzyl)spiro groups. |
| AID560139 | Antifungal activity against Candida glabrata isolate 22853 at 10 ug after 48 hrs by disk diffusion method | 2009 | Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7 | Hypersusceptibility to azole antifungals in a clinical isolate of Candida glabrata with reduced aerobic growth. |
| AID1156683 | Antifungal activity against Malassezia pachydermatis assessed as zone of inhibition at 1 mg/disc after 48 hrs incubation by disc diffusion assay | 2014 | European journal of medicinal chemistry, Aug-18, Volume: 83 | Synthesis of new class of spirocarbocycle derivatives by multicomponent domino reaction and their evaluation for antimicrobial, anticancer activity and molecular docking studies. |
| AID524791 | Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay | 2009 | Nature chemical biology, Oct, Volume: 5, Issue:10 | Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum. |
| AID415954 | Antimicrobial activity against Microsporum gypseum by micro-broth dilution method | 2009 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6 | Design, synthesis, and biological evaluation of novel 1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluorophenyl)-3-substituted benzylamino-2-propanols. |
| AID530956 | Antifungal activity against Aspergillus fumigatus ATCC 90906 after 5 days by CLSI method | 2008 | Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7 | Potent in vitro antifungal activities of naturally occurring acetylenic acids. |
| AID55188 | The compound was tested for antifungal activity against Cryptococcus neoformans MY1051 using agar dilution assay | 1987 | Journal of medicinal chemistry, Aug, Volume: 30, Issue:8 | Lysosomotropic agents. 7. Broad-spectrum antifungal activity of lysosomotropic detergents. |
| AID600778 | Fungicidal activity against Penicillium ochrochloron ATCC 9112 after 72 hrs | 2011 | Bioorganic & medicinal chemistry, May-15, Volume: 19, Issue:10 | Thiazole-based chalcones as potent antimicrobial agents. Synthesis and biological evaluation. |
| AID681378 | TP_TRANSPORTER: inhibition of Taurocholate uptake in NTCP-expressing HeLa cells | 1999 | The Journal of pharmacology and experimental therapeutics, Dec, Volume: 291, Issue:3 | Modulation by drugs of human hepatic sodium-dependent bile acid transporter (sodium taurocholate cotransporting polypeptide) activity. |
| AID624623 | Apparent permeability (Papp) from basolateral to apical side determined in MDR1-MDCKII cells | 2001 | The Journal of pharmacology and experimental therapeutics, Nov, Volume: 299, Issue:2 | Rational use of in vitro P-glycoprotein assays in drug discovery. |
| AID83861 | Effect on total serum cholesterol in male hamsters at a dose of 200 mg/kg orally administered for 14 days | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | Selective inhibition of mammalian lanosterol 14 alpha-demethylase: a possible strategy for cholesterol lowering. |
| AID717024 | Antifungal activity against Candida glabrata Osmangazi University clinical isolate after 24 hrs by microdilution susceptibility assay | 2012 | European journal of medicinal chemistry, Dec, Volume: 58 | Synthesis and biological evaluation of some hydrazone derivatives as new anticandidal and anticancer agents. |
| AID325035 | Antimicrobial activity against Candida albicans SC5314 after 24 hrs by broth macrodilution method | 2007 | Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5 | A Candida albicans petite mutant strain with uncoupled oxidative phosphorylation overexpresses MDR1 and has diminished susceptibility to fluconazole and voriconazole. |
| AID405034 | Antifungal activity against Sporothrix schenckii PSCC1 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by Sensititre YeastOne method | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods. |
| AID1467481 | Antifungal activity against Fusarium oxysporum after 48 to 72 hrs by microdilution method | 2017 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 27, Issue:14 | Synthesis, SAR and molecular docking studies of benzo[d]thiazole-hydrazones as potential antibacterial and antifungal agents. |
| AID456835 | Antifungal activity against Penicillium funiculosum ATCC 36839 after 72 hrs by serial sub-cultivation method | 2010 | Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1 | Novel 4-thiazolidinone derivatives as potential antifungal and antibacterial drugs. |
| AID374103 | Antimicrobial activity against Candida albicans ATCC 14053 at 100 ug/disk after 5 days by agar disk diffusion method | 2009 | European journal of medicinal chemistry, Apr, Volume: 44, Issue:4 | New acyclic nucleosides analogues as potential analgesic, anti-inflammatory, anti-oxidant and anti-microbial derived from pyrimido[4,5-b]quinolines. |
| AID336892 | Antifungal activity against Microsporum canis after 2 to 4 days | |||
| AID315660 | Inhibition of recombinant CYP2C9 at 10 uM | 2008 | Bioorganic & medicinal chemistry, Feb-15, Volume: 16, Issue:4 | Synthesis, biological evaluation and molecular modelling studies of methyleneimidazole substituted biaryls as inhibitors of human 17alpha-hydroxylase-17,20-lyase (CYP17). Part I: Heterocyclic modifications of the core structure. |
| AID594131 | Antimicrobial activity against Bacillus megaterium ATCC 9885 after 24 hrs by agar well diffusion method | 2011 | European journal of medicinal chemistry, May, Volume: 46, Issue:5 | Synthesis, antimicrobial, antioxidant, anti-hemolytic and cytotoxic evaluation of new imidazole-based heterocycles. |
| AID531206 | Antifungal activity against Candida albicans ATCC 60193 after 48 hrs by CLSI method | 2008 | Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7 | Potent in vitro antifungal activities of naturally occurring acetylenic acids. |
| AID39390 | In vitro evaluation of minimum inhibitory concentration against Aspergillus flavus 19 | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20 | Synthesis and antifungal activity of new azole derivatives containing an N-acylmorpholine ring. |
| AID588212 | Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents | 2010 | Chemical research in toxicology, Jan, Volume: 23, Issue:1 | Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species. |
| AID574256 | Antifungal activity against 10'3 cells/ml Candida albicans SC5314 by NCCLS method | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | Cell density and cell aging as factors modulating antifungal resistance of Candida albicans biofilms. |
| AID574253 | Antifungal activity against 24 hrs cultures of 10'7 cells/ml wild-type Candida albicans BF-1 biofilms by XTT reduction assay | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | Cell density and cell aging as factors modulating antifungal resistance of Candida albicans biofilms. |
| AID1557073 | Antifungal activity against Candida albicans SN152 assessed as zone inhibition at 25 ug incubated for 24 hrs by disk diffusion method | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Antifungal activity, mode of action variability, and subcellular distribution of coumarin-based antifungal azoles. |
| AID333564 | Antifungal activity against Candida albicans ATCC 10231 | 2004 | Journal of natural products, Nov, Volume: 67, Issue:11 | (2S,3R)-2-aminododecan-3-ol, a new antifungal agent from the ascidian Clavelina oblonga. |
| AID100102 | Dissociation constant was determined in vitro using rat pituitary membranes and [125I]-leuprolide as radioligand, at concentration 3.16*10e-6 M | 1989 | Journal of medicinal chemistry, Sep, Volume: 32, Issue:9 | LH-RH antagonists: design and synthesis of a novel series of peptidomimetics. |
| AID208219 | Inhibition of Trichosporon beigelli 1188 for 24 hours in vitro. | 2001 | Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17 | 3-Phenyl-5-acyloxymethyl-2H,5H-furan-2-ones: synthesis and biological activity of a novel group of potential antifungal drugs. |
| AID362809 | Antifungal activity against Fusarium solani at 200 ug after 48 hrs by agar disc-diffusion method | 2008 | European journal of medicinal chemistry, May, Volume: 43, Issue:5 | Synthesis and antimicrobial activity of novel sulfone-linked bis heterocycles. |
| AID363938 | Antimicrobial activity against Cryptococcus neoformans IM 042074 isolate at 6.25 ug/ml after 48 hrs | 2008 | Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17 | In vitro antifungal activity of polyfunctionalized 2-(hetero)arylquinolines prepared through imino Diels-Alder reactions. |
| AID362238 | Inhibition of hepatic CYP2D6 expressed in insect microsomes at 1 uM | 2008 | Bioorganic & medicinal chemistry, Aug-15, Volume: 16, Issue:16 | Synthesis, biological evaluation, and molecular modeling studies of methylene imidazole substituted biaryls as inhibitors of human 17alpha-hydroxylase-17,20-lyase (CYP17)--part II: Core rigidification and influence of substituents at the methylene bridge. |
| AID2977 | Inhibition of cytochrome P450 progesterone 2-alpha-hydroxylase | 1992 | Journal of medicinal chemistry, Jul-24, Volume: 35, Issue:15 | Stereoisomers of ketoconazole: preparation and biological activity. |
| AID436297 | Inhibition of human recombinant aromatase | 2008 | Journal of natural products, Nov, Volume: 71, Issue:11 | Monodictyochromes A and B, dimeric xanthone derivatives from the marine algicolous fungus Monodictys putredinis. |
| AID1443980 | Inhibition of human BSEP expressed in fall armyworm sf9 cell plasma membrane vesicles assessed as reduction in vesicle-associated [3H]-taurocholate transport preincubated for 10 mins prior to ATP addition measured after 15 mins in presence of [3H]-tauroch | 2010 | Toxicological sciences : an official journal of the Society of Toxicology, Dec, Volume: 118, Issue:2 | Interference with bile salt export pump function is a susceptibility factor for human liver injury in drug development. |
| AID406860 | Antimicrobial activity against Candida albicans SC5314 dissociated biofilms at cell density of 10'8 cells/ml after 48 hrs by XTT assay | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | Role for cell density in antifungal drug resistance in Candida albicans biofilms. |
| AID635009 | Antifungal activity against Aspergillus niger NCIM 596 assessed as zone of inhibition at 200 ug/disc after 48 hrs by disk diffusion method | 2012 | European journal of medicinal chemistry, Jan, Volume: 47, Issue:1 | Synthesis, antimicrobial, antimycobacterial and structure-activity relationship of substituted pyrazolo-, isoxazolo-, pyrimido- and mercaptopyrimidocyclohepta[b]indoles. |
| AID681128 | TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1b-expressing LLC-PK1 cells | 2003 | Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9 | Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery. |
| AID566957 | Antifungal activity against Cryptococcus neoformans ATCC 32264 assessed as inhibition of fungal growth at 12.5 uM after 48 hrs by microplate analysis | 2011 | European journal of medicinal chemistry, Jan, Volume: 46, Issue:1 | Penetratin analogues acting as antifungal agents. |
| AID362136 | Inhibition of human recombinant CYP3A4 expressed in insect microsomes | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16 | Overcoming undesirable CYP1A2 inhibition of pyridylnaphthalene-type aldosterone synthase inhibitors: influence of heteroaryl derivatization on potency and selectivity. |
| AID774145 | Inhibition of CYP2D6 in human liver microsomes assessed as bufuralol hydroxylation to 4'-hydroxybufuralol at 1 uM after 10 mins relative to control | 2013 | Journal of medicinal chemistry, Oct-10, Volume: 56, Issue:19 | Rational development of 4-aminopyridyl-based inhibitors targeting Trypanosoma cruzi CYP51 as anti-chagas agents. |
| AID1130386 | Antifungal activity against Streptococcus pyogenes assessed as growth inhibition in sabouraud broth after 14 days | 1979 | Journal of medicinal chemistry, Aug, Volume: 22, Issue:8 | Antimycotic imidazoles. part 4. Synthesis and antifungal activity of ketoconazole, a new potent orally active broad-spectrum antifungal agent. |
| AID1443989 | Inhibition of recombinant human BSEP expressed in baculovirus infected sf9 cell plasma membrane vesicles assessed as reduction in ATP-dependent [3H]-taurocholate uptake in to vesicles preincubated for 10 mins followed by ATP addition measured after 10 to | 2014 | Hepatology (Baltimore, Md.), Sep, Volume: 60, Issue:3 | Human drug-induced liver injury severity is highly associated with dual inhibition of liver mitochondrial function and bile salt export pump. |
| AID511043 | Antimicrobial activity against Aspergillus niger NCIM 596 at 200 ug/disk after 48 hrs by agar disc-diffusion method | 2010 | European journal of medicinal chemistry, Sep, Volume: 45, Issue:9 | Synthesis and bioassay of aminosulfonyl-1,3,4-oxadiazoles and their interconversion to 1,3,4-thiadiazoles. |
| AID625286 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID283200 | Susceptibility of polyene-resistant Candida glabrata 21229 isolate at 15 ug by disk diffusion method | 2007 | Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3 | Reduced susceptibility to polyenes associated with a missense mutation in the ERG6 gene in a clinical isolate of Candida glabrata with pseudohyphal growth. |
| AID575106 | Antifungal activity against Madurella mycetomatis isolate 36 by XTT assay | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Madurella mycetomatis is not susceptible to the echinocandin class of antifungal agents. |
| AID1456583 | Antifungal activity against Microsporum gypseum isolate cmccftla by micro-broth dilution method | 2017 | Bioorganic & medicinal chemistry letters, 05-15, Volume: 27, Issue:10 | Design, synthesis, and in vitro evaluation of novel antifungal triazoles. |
| AID1275150 | Antifungal activity against Aspergillus parasiticus NRRL 465 after 72 hrs by broth microdilution method | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Synthesis and biological evaluation of new naphthalene substituted thiosemicarbazone derivatives as potent antifungal and anticancer agents. |
| AID448519 | Antimicrobial activity against Alternaria alternata after 24 hrs by serial dilution method | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11 | Synthesis of some novel pyrazolo[3,4-b]pyridine and pyrazolo[3,4-d]pyrimidine derivatives bearing 5,6-diphenyl-1,2,4-triazine moiety as potential antimicrobial agents. |
| AID1061000 | Antimicrobial activity against Candida tropicalis CGMCC2.3967 after 48 hrs by twofold serial microdilution method | 2014 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1 | Synthesis and biological evaluation of novel N-substituted 1H-dibenzo[a,c]carbazole derivatives of dehydroabietic acid as potential antimicrobial agents. |
| AID1491276 | Inhibition of CYP3A4 in human liver microsomes using midazolam as substrate preincubated for 10 mins followed by NADPH addition measured after 10 mins by LC/MS/MS analysis | 2017 | European journal of medicinal chemistry, Sep-08, Volume: 137 | Design, synthesis and evaluation of aromatic heterocyclic derivatives as potent antifungal agents. |
| AID189041 | Percent reduction in recovery of Candida albicans (experimental vaginitis) in rats at 10 mg/kg (po) | 1983 | Journal of medicinal chemistry, Mar, Volume: 26, Issue:3 | Synthesis of (E)-1-(5-chlorothien-2-yl)-2-(1H-imidazol-1-yl)ethanone 2,6-dichlorophenylhydrazone hydrochloride, a novel, orally active antifungal agent. |
| AID381186 | Antifungal activity against amphotericin-resistant Candida tropicalis after 24 to 72 hrs by disk diffusion method | 1999 | Journal of natural products, Sep, Volume: 62, Issue:9 | Antimicrobial and antitumor activities of mycosporulone. |
| AID53739 | Binding affinity was measured on Cytochrome P450 19A1 | 1990 | Journal of medicinal chemistry, Nov, Volume: 33, Issue:11 | Mechanism and inhibition of cytochrome P-450 aromatase. |
| AID1218831 | Inactivation of recombinant CYP3A4 (unknown origin) using midazolam as substrate assessed as recovery of enzyme activity at 1 uM preincubated for 5 mins followed by dialysis measured after 24 hrs | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7 | Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme. |
| AID553069 | Inhibition of human placental microsomes CYP19 at 500 nM using androstenedione substrate | 2011 | ACS medicinal chemistry letters, Jan-13, Volume: 2, Issue:1 | First Selective CYP11B1 Inhibitors for the Treatment of Cortisol-Dependent Diseases. |
| AID363717 | Antifungal activity against Trichophyton rubrum C110 after 48 hrs by broth microdilution technique | 2008 | Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17 | In vitro antifungal activity of polyfunctionalized 2-(hetero)arylquinolines prepared through imino Diels-Alder reactions. |
| AID408340 | Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique | 2008 | Bioorganic & medicinal chemistry, Jun-01, Volume: 16, Issue:11 | Support vector machines classification of hERG liabilities based on atom types. |
| AID1472634 | Inhibition of CYP3A4 in human liver microsomes using testosterone as substrate upto 10 uM after 5 mins in presence of NADPH by LC-MS/MS analysis | 2018 | Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1 | Novel Terminal Bipheny-Based Diapophytoene Desaturases (CrtN) Inhibitors as Anti-MRSA/VISR/LRSA Agents with Reduced hERG Activity. |
| AID488639 | Antimicrobial activity against Candida albicans ATCC 10231 by broth dilution method | 2010 | Journal of natural products, Jun-25, Volume: 73, Issue:6 | Alkaloids from the bark of Guatteria hispida and their evaluation as antioxidant and antimicrobial agents. |
| AID667056 | Antifungal activity against Penicillium chrysogenum at 100 ug/ml after 48 hrs by agar well diffusion method | 2012 | European journal of medicinal chemistry, Aug, Volume: 54 | Synthesis, antimicrobial and cytotoxic activities of sulfone linked bis heterocycles. |
| AID261015 | Inhibitory activity against Candida krusei | 2006 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 16, Issue:4 | Novel endoperoxides: synthesis and activity against Candida species. |
| AID652428 | Inhibition of human CYP11B1 expressed in hamster V79 MZ cells using [3H] 11 deoxycorticosterone as substrate by HPLC radioflow detector | 2011 | ACS medicinal chemistry letters, Aug-11, Volume: 2, Issue:8 | Optimization of the First Selective Steroid-11β-hydroxylase (CYP11B1) Inhibitors for the Treatment of Cortisol Dependent Diseases. |
| AID530918 | Antifungal activity against Candida albicans ATCC 90028 at 9.4 uM after 48 hrs by CLSI method | 2008 | Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7 | Potent in vitro antifungal activities of naturally occurring acetylenic acids. |
| AID486237 | Antifungal activity against Cryptococcus neoformans ATCC 32264 after 48 hrs | 2010 | European journal of medicinal chemistry, Jun, Volume: 45, Issue:6 | Naftifine-analogues as anti-Trypanosoma cruzi agents. |
| AID407022 | Antimicrobial activity against Chk1 deficient Candida albicans CHK21 intact biofilms after 48 hrs by XTT assay | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | Role for cell density in antifungal drug resistance in Candida albicans biofilms. |
| AID555139 | Antimicrobial activity against Candida krusei ATCC 6258 by CLSI M27-A2 broth microdilution method | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Fenticonazole activity measured by the methods of the European Committee on Antimicrobial Susceptibility Testing and CLSI against 260 Candida vulvovaginitis isolates from two European regions and annotations on the prevalent genotypes. |
| AID456686 | Antifungal activity against Cryptococcus neoformans ATCC 32264 assessed as inhibition of fungal growth at 6.25 uM after 48 hrs by microbroth dilution method | 2010 | Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1 | New small-size peptides possessing antifungal activity. |
| AID407014 | Antimicrobial activity against Cdr1, Cdr2 and Mdr1 deficient Candida albicans DSY1050 at planktonic cell density of 10'8 cells/ml after 48 hrs by XTT assay | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | Role for cell density in antifungal drug resistance in Candida albicans biofilms. |
| AID1079946 | Presence of at least one case with successful reintroduction. [column 'REINT' in source] | |||
| AID340964 | Antifungal activity against Pichia anomala isolates from grapes by NCCLS M27-A2 method | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8 | Cross-resistance to medical and agricultural azole drugs in yeasts from the oropharynx of human immunodeficiency virus patients and from environmental Bavarian vine grapes. |
| AID47582 | Evaluation of In vitro antifungal activity against Candida albicans 406 by broth macro dilution method | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20 | Synthesis and antifungal activity of new azole derivatives containing an N-acylmorpholine ring. |
| AID765641 | Fungistatic activity against Saccharomyces cerevisiae after 24 hrs by two-fold serial dilution assay | 2013 | European journal of medicinal chemistry, Sep, Volume: 67 | Synthesis of thiosemicarbazones derived from N-(4-hippuric acid)thiosemicarbazide and different carbonyl compounds as antimicrobial agents. |
| AID287381 | Antifungal activity against Kluyveromyces fragilis after 24 hrs by disk diffusion method | 2007 | European journal of medicinal chemistry, Feb, Volume: 42, Issue:2 | Synthesis, characterization and antimicrobial activity of Fe(II), Zn(II), Cd(II) and Hg(II) complexes with 2,6-bis(benzimidazol-2-yl) pyridine ligand. |
| AID606218 | Antifungal activity against Fonsecaea compacta by micro-broth dilution method | 2011 | European journal of medicinal chemistry, Jul, Volume: 46, Issue:7 | Design, synthesis and antifungal activities of novel 1,2,4-triazole derivatives. |
| AID334235 | Antimicrobial activity against Microsporum gypseum NCPF 40 after 10 days by microdilution technique | 2002 | Journal of natural products, Apr, Volume: 65, Issue:4 | Antimicrobial activities of a new schizozygane indoline alkaloid from Schizozygia coffaeoides and the revised structure of isoschizogaline. |
| AID456682 | Antifungal activity against Cryptococcus neoformans ATCC 32264 assessed as inhibition of fungal growth at 100 uM after 48 hrs by microbroth dilution method | 2010 | Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1 | New small-size peptides possessing antifungal activity. |
| AID1319257 | Inhibition of CYP3A4 in human liver microsomes using midazolam as substrate assessed as reduction in 1-OH-midazolam formation at 0.005 uM by LC/MS/MS analysis | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18 | Identification of (R)-(2-Chloro-3-(trifluoromethyl)phenyl)(1-(5-fluoropyridin-2-yl)-4-methyl-6,7-dihydro-1H-imidazo[4,5-c]pyridin-5(4H)-yl)methanone (JNJ 54166060), a Small Molecule Antagonist of the P2X7 receptor. |
| AID330530 | Antifungal activity against Candida parapsilosis infected cyclophosphamide-immunocompromized Crl:CD1(ICR) mouse assessed as fungal density in lung at 0.5 mg/kg, po for 5 days measured on day 12 in presence beauvericin | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Mar-13, Volume: 104, Issue:11 | High-throughput synergy screening identifies microbial metabolites as combination agents for the treatment of fungal infections. |
| AID689077 | Antibacterial activity against Bacillus megaterium assessed as zone of inhibition at 0.05 mg by agar diffusion method | 2012 | Journal of natural products, Sep-28, Volume: 75, Issue:9 | Sinularosides A and B, bioactive 9,11-secosteroidal glycosides from the South China Sea soft coral Sinularia humilis Ofwegen. |
| AID481913 | Antifungal activity against Candida glabrata NRRL Y-65 at 15 ug in 6 mm disk after 10 hrs by disc-diffusion assay | 2010 | Journal of natural products, May-28, Volume: 73, Issue:5 | Chemical epigenetics alters the secondary metabolite composition of guttate excreted by an atlantic-forest-soil-derived Penicillium citreonigrum. |
| AID1223623 | Inhibition of CYP3A4 activity in human liver microsomes using nifedipine as a substrate by LC/MS analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4 | Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID1456580 | Antifungal activity against Candida glabrata isolate 537 by micro-broth dilution method | 2017 | Bioorganic & medicinal chemistry letters, 05-15, Volume: 27, Issue:10 | Design, synthesis, and in vitro evaluation of novel antifungal triazoles. |
| AID1171995 | Antifungal activity against Candida albicans MTCC 227 assessed as inhibition of visual growth after 48 to 72 hrs | 2015 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2 | Facile and diastereoselective synthesis of 3,2'-spiropyrrolidine-oxindoles derivatives, their molecular docking and antiproliferative activities. |
| AID554713 | Antimicrobial activity against Candida krusei NZCDC 89.021 after 48 hrs by CLSI method | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2 | Abc1p is a multidrug efflux transporter that tips the balance in favor of innate azole resistance in Candida krusei. |
| AID311900 | Toxicity against brine shrimp by lethality test | 2007 | Journal of natural products, Dec, Volume: 70, Issue:12 | Bioactive polychlorinated bibenzyls from the liverwort Riccardia polyclada. |
| AID386887 | Antimicrobial activity against Candida albicans ATCC 2091 by cup plate method | 2008 | European journal of medicinal chemistry, Oct, Volume: 43, Issue:10 | Condensed bridgehead nitrogen heterocyclic system: synthesis and pharmacological activities of 1,2,4-triazolo-[3,4-b]-1,3,4-thiadiazole derivatives of ibuprofen and biphenyl-4-yloxy acetic acid. |
| AID394834 | Inhibition of Trypanosoma cruzi recombinant sterol 14-alpha-demethylase assessed as drug/enzyme molar ratio required to produce 50 percent decrease in turnover number | 2009 | Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6 | Rational modification of a candidate cancer drug for use against Chagas disease. |
| AID437542 | Inhibition of human recombinant CYP3A4 assessed as biotransformation of 7-benzyloxyquinoline to 7-hydroxyquinoline measured every 15 mins by fluorescence intensity analysis | 2009 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19 | Structure-activity studies on seco-pancratistatin analogs: potent inhibitors of human cytochrome P450 3A4. |
| AID1160913 | Inhibition of human MBP-tagged CYP24A1 expressed in Escherichia coli using 1,25(OH)2D3 substrate in presence of bovine adrenodoxin, adrenodoxin reductase and NADPH incubated at 37 degC for 25 mins by HPLC method | 2014 | Journal of medicinal chemistry, Sep-25, Volume: 57, Issue:18 | Small-molecule inhibitors of 25-hydroxyvitamin D-24-hydroxylase (CYP24A1): synthesis and biological evaluation. |
| AID367161 | Antimicrobial activity against Aspergillus fumigatus by broth microdilution method | 2009 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 19, Issue:3 | Synthesis and antifungal activity of 1,2,3-triazole containing fluconazole analogues. |
| AID262558 | Antifungal activity against Epidermophyton floccosum | 2006 | Journal of medicinal chemistry, Apr-20, Volume: 49, Issue:8 | Structure-based optimization of azole antifungal agents by CoMFA, CoMSIA, and molecular docking. |
| AID549046 | Antifungal activity against Candida albicans CA3 after 48 hrs by broth microdilution method | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | In vitro activities of retigeric acid B alone and in combination with azole antifungal agents against Candida albicans. |
| AID343560 | Selectivity index, ratio of IC50 for mouse J774 cells to IC50 for epimastigotes of Trypanosoma cruzi Tulahuen 2 | 2008 | Bioorganic & medicinal chemistry, Jul-15, Volume: 16, Issue:14 | New trypanocidal hybrid compounds from the association of hydrazone moieties and benzofuroxan heterocycle. |
| AID613255 | Antibacterial activity against Escherichia coli ATCC 11303 after 24 hrs by NCCLS M7-A6 broth dilution method | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Design, synthesis and antimicrobial activity of chiral 2-(substituted-hydroxyl)-3-(benzo[d]oxazol-5-yl)propanoic acid derivatives. |
| AID404140 | Antifungal activity against Trichophyton mentagrophytes var. interdigitale CPCM 06.99 | 2005 | Journal of natural products, Nov, Volume: 68, Issue:11 | Extraction, hemisynthesis, and synthesis of canthin-6-one analogues. Evaluation of their antifungal activities. |
| AID632005 | Toxicity in CBA mouse infected with Leishmania amazonensis MHOM/ BR/77/LTB0016 assessed as change in neutrophils count at 50 mg/kg, po qd for 30 days administered 4 week post infection measured up to week 21 | 2011 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 21, Issue:24 | Synthesis and antileishmanial evaluation of 1-aryl-4-(4,5-dihydro-1H-imidazol-2-yl)-1H-pyrazole derivatives. |
| AID1332943 | Antifungal activity against Aspergillus flavus MTCC 1884 at 200 ug/mL incubated at 4 degC for 24 hrs followed by subsequent incubation at 37.5 degC for 3 days by poisoned food method | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Synthesis, antimicrobial activity and advances in structure-activity relationships (SARs) of novel tri-substituted thiazole derivatives. |
| AID481668 | Antifungal activity against Candida glabrata clinical isolate 2 after 24 hrs by broth microdilution assay | 2010 | European journal of medicinal chemistry, May, Volume: 45, Issue:5 | Synthesis and the selective antifungal activity of 5,6,7,8-tetrahydroimidazo[1,2-a]pyridine derivatives. |
| AID50310 | Tested for minimum subinhibitory concentration against Candida krusei 132 (C.k) at pH 6.5. | 1994 | Journal of medicinal chemistry, Jun-24, Volume: 37, Issue:13 | Derivatives of a novel cyclopeptolide. 1. Synthesis, antifungal activity, and structure-activity relationships. |
| AID323061 | Antifungal activity against Aspergillus fumigatus ATCC 26934 by micro-broth dilution method | 2008 | Bioorganic & medicinal chemistry, Jan-15, Volume: 16, Issue:2 | Antifungal and cytotoxic activities of some N-substituted aniline derivatives bearing a hetaryl fragment. |
| AID283206 | Antimicrobial activity against polyene-resistant Candida glabrata 21229 isolate by E-test | 2007 | Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3 | Reduced susceptibility to polyenes associated with a missense mutation in the ERG6 gene in a clinical isolate of Candida glabrata with pseudohyphal growth. |
| AID213657 | Growth inhibitory activity against Trypanosoma cruzi (Epimastigote) | 1998 | Bioorganic & medicinal chemistry letters, Nov-17, Volume: 8, Issue:22 | Growth inhibitory effect of juvenile hormone analogues on epimastigotes of Trypanosoma cruzi. |
| AID1557080 | Antifungal activity against Candida glabrata 192 assessed as reduction in fungal cell growth incubated for 24 hrs by MTT based broth double dilution method | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Antifungal activity, mode of action variability, and subcellular distribution of coumarin-based antifungal azoles. |
| AID1130397 | Antifungal activity against Candida albicans B2630 infected in ovariectomized and hysterectomized Wistar rat vaginal candidosis model at 5 mg/kg, po for 5 days by prophylactic treatment | 1979 | Journal of medicinal chemistry, Aug, Volume: 22, Issue:8 | Antimycotic imidazoles. part 4. Synthesis and antifungal activity of ketoconazole, a new potent orally active broad-spectrum antifungal agent. |
| AID1304742 | Antifungal activity against Trichophyton mentagrophytes measured after 7 days by serial dilution method | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7 | Discovery of Potent Benzofuran-Derived Diapophytoene Desaturase (CrtN) Inhibitors with Enhanced Oral Bioavailability for the Treatment of Methicillin-Resistant Staphylococcus aureus (MRSA) Infections. |
| AID574260 | Antifungal activity against 24 hrs cultures of 10'7 cells/ml Candida albicans BF-1 planktonic cells by XTT reduction method | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | Cell density and cell aging as factors modulating antifungal resistance of Candida albicans biofilms. |
| AID406857 | Antimicrobial activity against Candida albicans SC5314 at planktonic cell density of 10'3 cells/ml after 48 hrs by XTT assay | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | Role for cell density in antifungal drug resistance in Candida albicans biofilms. |
| AID54872 | In vitro antifungal activity against Cryptococcus neoformans | 1984 | Journal of medicinal chemistry, Jul, Volume: 27, Issue:7 | Antimycotic azoles. 7. Synthesis and antifungal properties of a series of novel triazol-3-ones. |
| AID363948 | Antimicrobial activity against Cryptococcus neoformans IM 00319 isolate at 6.25 ug/ml after 48 hrs | 2008 | Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17 | In vitro antifungal activity of polyfunctionalized 2-(hetero)arylquinolines prepared through imino Diels-Alder reactions. |
| AID702956 | Plasma protein binding in human plasma at 10 uM | 2012 | Journal of medicinal chemistry, Jun-28, Volume: 55, Issue:12 | Identification, synthesis, and biological evaluation of the metabolites of 3-amino-6-(3'-aminopropyl)-5H-indeno[1,2-c]isoquinoline-5,11-(6H)dione (AM6-36), a promising rexinoid lead compound for the development of cancer chemotherapeutic and chemopreventi |
| AID407012 | Antimicrobial activity against fluconazole-resistant Candida albicans FH5 intact biofilms after 48 hrs by XTT assay | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | Role for cell density in antifungal drug resistance in Candida albicans biofilms. |
| AID674801 | Antifungal activity against wild type Aspergillus fumigatus Af293 after 48 hrs by microtiter broth dilution method | 2012 | European journal of medicinal chemistry, Sep, Volume: 55 | Laurene-type sesquiterpenes from the Red Sea red alga Laurencia obtusa as potential antitumor-antimicrobial agents. |
| AID600779 | Fungicidal activity against Penicillium funiculosum ATCC 36839 after 72 hrs | 2011 | Bioorganic & medicinal chemistry, May-15, Volume: 19, Issue:10 | Thiazole-based chalcones as potent antimicrobial agents. Synthesis and biological evaluation. |
| AID574250 | Antifungal activity against 10'8 cells/ml Candida albicans ATCC 90028 planktonic cells by XTT reduction assay | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | Cell density and cell aging as factors modulating antifungal resistance of Candida albicans biofilms. |
| AID454771 | Cytotoxicity against mouse J774 cells after 48 hrs by MTT assay | 2009 | Bioorganic & medicinal chemistry, Nov-01, Volume: 17, Issue:21 | 5-Nitrofuranes and 5-nitrothiophenes with anti-Trypanosoma cruzi activity and ability to accumulate squalene. |
| AID50120 | Tested for minimum subinhibitory concentration against Candida guilliermondii 80 (C.g) at pH 6.5. | 1994 | Journal of medicinal chemistry, Jun-24, Volume: 37, Issue:13 | Derivatives of a novel cyclopeptolide. 1. Synthesis, antifungal activity, and structure-activity relationships. |
| AID688634 | Antifungal activity against Aspergillus niger at 50 ug after 48 hrs by agar well diffusion method | 2011 | European journal of medicinal chemistry, Nov, Volume: 46, Issue:11 | Synthesis and antimicrobial activity of amido linked pyrrolyl and pyrazolyl-oxazoles, thiazoles and imidazoles. |
| AID244794 | Antifungal activity to cause 99% reduction of surviving cells range is equal to 8-32 | 2004 | Journal of medicinal chemistry, Jul-29, Volume: 47, Issue:16 | Imidazole analogues of fluoxetine, a novel class of anti-Candida agents. |
| AID249325 | Minimum inhibitory concentration to inhibit 90% of the isolates | 2004 | Journal of medicinal chemistry, Jul-29, Volume: 47, Issue:16 | Imidazole analogues of fluoxetine, a novel class of anti-Candida agents. |
| AID604260 | Antibacterial activity against Candida albicans ATCC 10231 after 48 hrs by MTT colorimetric method | 2011 | Bioorganic & medicinal chemistry, Jul-01, Volume: 19, Issue:13 | 4-alkoxy-3-arylfuran-2(5H)-ones as inhibitors of tyrosyl-tRNA synthetase: synthesis, molecular docking and antibacterial evaluation. |
| AID530984 | Antifungal activity against Aspergillus niger ATCC 16404 at 9.4 uM after 48 hrs by CLSI method | 2008 | Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7 | Potent in vitro antifungal activities of naturally occurring acetylenic acids. |
| AID319753 | Antimicrobial activity against Cryptococcus neoformans ATCC 32609 | 2008 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 18, Issue:11 | Synthesis and SAR studies of biaryloxy-substituted triazoles as antifungal agents. |
| AID1247099 | Antifungal activity against Malassezia pachydermatis after 48 to 72 hrs by two fold serial dilution method | 2015 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19 | Synthesis of BF₃ catalyzed Mannich derivatives with excellent ee from phenylpropanolamine, study of their antimicrobial activity and molecular docking. |
| AID555134 | Antimicrobial activity against Candida glabrata by CLSI M27-A2 broth microdilution method | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Fenticonazole activity measured by the methods of the European Committee on Antimicrobial Susceptibility Testing and CLSI against 260 Candida vulvovaginitis isolates from two European regions and annotations on the prevalent genotypes. |
| AID678713 | Inhibition of human CYP2C9 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-methoxy-4-trifluoromethylcoumarin-3-acetic acid as substrate after 30 mins | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
| AID635007 | Antifungal activity against Curvularia lunata NCIM 716 assessed as zone of inhibition at 200 ug/disc after 48 hrs by disk diffusion method | 2012 | European journal of medicinal chemistry, Jan, Volume: 47, Issue:1 | Synthesis, antimicrobial, antimycobacterial and structure-activity relationship of substituted pyrazolo-, isoxazolo-, pyrimido- and mercaptopyrimidocyclohepta[b]indoles. |
| AID599146 | Antibacterial activity against Bacillus subtilis after 24 hrs by MTT assay | 2008 | European journal of medicinal chemistry, Mar, Volume: 43, Issue:3 | Synthesis, crystal structure and antimicrobial activity of deoxybenzoin derivatives from genistein. |
| AID270825 | Inhibition of rat testis 17,20 lyase component of P450-17alpha | 2006 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 16, Issue:18 | Synthesis, biochemical evaluation and rationalisation of the inhibitory activity of a range of 4-substituted phenyl alkyl imidazole-based inhibitors of the enzyme complex 17alpha-hydroxylase/17,20-lyase (P450(17alpha)). |
| AID48084 | Evaluation of In vitro antifungal activity against yeasts by broth macro dilution method | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20 | Synthesis and antifungal activity of new azole derivatives containing an N-acylmorpholine ring. |
| AID1055945 | Antifungal activity against Candida albicans ATCC 10231 after 48 hrs | 2013 | Journal of natural products, Nov-22, Volume: 76, Issue:11 | Hytramycins V and I, anti-Mycobacterium tuberculosis hexapeptides from a Streptomyces hygroscopicus strain. |
| AID640966 | Antifungal activity against Candida albicans NCIM 3102 after 48 hrs by agar well diffusion assay | 2012 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2 | Synthesis, characterization and in vitro biological evaluation of some novel diarylsulfonylureas as potential cytotoxic and antimicrobial agents. |
| AID1467480 | Antifungal activity against Fusarium moniliforme after 48 to 72 hrs by microdilution method | 2017 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 27, Issue:14 | Synthesis, SAR and molecular docking studies of benzo[d]thiazole-hydrazones as potential antibacterial and antifungal agents. |
| AID530954 | Antifungal activity against Aspergillus niger ATCC 16404 after 5 days by CLSI method | 2008 | Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7 | Potent in vitro antifungal activities of naturally occurring acetylenic acids. |
| AID696542 | Antifungal activity against Aspergillus niger ATCC 9029 after 48 hrs by broth microdilution technique | 2012 | Bioorganic & medicinal chemistry, Nov-01, Volume: 20, Issue:21 | Synthesis and antifungal activity of diverse C-2 pyridinyl and pyridinylvinyl substituted quinolines. |
| AID1171985 | Antifungal activity against Malassezia pachydermatis assessed as zone of inhibition at 1 mg/disc after 48 hrs by disc diffusion method | 2015 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2 | Facile and diastereoselective synthesis of 3,2'-spiropyrrolidine-oxindoles derivatives, their molecular docking and antiproliferative activities. |
| AID723709 | Antifungal activity against Trichoderma viride IAM 5061 after 72 hrs by serial dilution technique | 2013 | Bioorganic & medicinal chemistry, Jan-15, Volume: 21, Issue:2 | Synthesis and biological evaluation of some 5-arylidene-2-(1,3-thiazol-2-ylimino)-1,3-thiazolidin-4-ones as dual anti-inflammatory/antimicrobial agents. |
| AID336891 | Antifungal activity against Aspergillus fumigatus MSU-SM 920 after 2 to 4 days | |||
| AID582802 | Antifungal activity against Candida albicans isolate 1008 harboring ERG3 K97E, L193P, V237A, A351V, A353T and ERG11 E266D mutant genes by broth microdilution method | 2010 | Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11 | Identification and characterization of four azole-resistant erg3 mutants of Candida albicans. |
| AID429270 | Antifungal activity against Candida albicans at 1000 ug/ml after 72 hrs by agar diffusion method | 2009 | European journal of medicinal chemistry, Aug, Volume: 44, Issue:8 | Mono and bis-6-arylbenzimidazo[1,2-c]quinazolines: a new class of antimicrobial agents. |
| AID566950 | Antifungal activity against Candida albicans ATCC 10231 assessed as inhibition of fungal growth at 25 uM after 24 hrs by microplate analysis | 2011 | European journal of medicinal chemistry, Jan, Volume: 46, Issue:1 | Penetratin analogues acting as antifungal agents. |
| AID1263194 | Cytotoxicity against human MCF7 cells as growth inhibition at 50 uM | 2015 | Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24 | Synthesis and activity of novel 16-dehydropregnenolone acetate derivatives as inhibitors of type 1 5α-reductase and on cancer cell line SK-LU-1. |
| AID363759 | Antimicrobial activity against Candida tropicalis C131 isolate at 6.25 ug/ml after 24 hrs | 2008 | Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17 | In vitro antifungal activity of polyfunctionalized 2-(hetero)arylquinolines prepared through imino Diels-Alder reactions. |
| AID47889 | Evaluation of In vitro antifungal activity against Candida parapsilosis C292 by broth macro dilution method | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20 | Synthesis and antifungal activity of new azole derivatives containing an N-acylmorpholine ring. |
| AID1165073 | Selectivity ratio of Ki for mouse CYP27B1 to Ki for N-terminally MBP-fused human CYP24A1 | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | Novel styryl-indoles as small molecule inhibitors of 25-hydroxyvitamin D-24-hydroxylase (CYP24A1): Synthesis and biological evaluation. |
| AID563612 | Effect on sterol composition in Candida albicans isolate 14 expressing wild type erg11 and erg5 assessed as 14 -Methylergosta-8,24(28)-dien-3beta,6alpha-diol level after 2 hrs by gas chromatography | 2010 | Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9 | A clinical isolate of Candida albicans with mutations in ERG11 (encoding sterol 14alpha-demethylase) and ERG5 (encoding C22 desaturase) is cross resistant to azoles and amphotericin B. |
| AID53214 | Tested for inhibitory activity against Cytochrome P450 17 from human testicular microsomes | 2000 | Journal of medicinal chemistry, Nov-16, Volume: 43, Issue:23 | Synthesis and evaluation of 17-aliphatic heterocycle-substituted steroidal inhibitors of 17alpha-hydroxylase/C17-20-lyase (P450 17). |
| AID1209973 | Inhibition of CYP2D6 in human liver microsomes using dextromethorphan as substrate after 8 mins by LC-MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5 | Identifying a selective substrate and inhibitor pair for the evaluation of CYP2J2 activity. |
| AID774149 | Inhibition of CYP2C9 in human liver microsomes assessed as tolbutamide hydroxylation to hydroxytolbutamide at 1 uM after 10 mins relative to control | 2013 | Journal of medicinal chemistry, Oct-10, Volume: 56, Issue:19 | Rational development of 4-aminopyridyl-based inhibitors targeting Trypanosoma cruzi CYP51 as anti-chagas agents. |
| AID270824 | Inhibition of rat testis 17,20 lyase component of P450-17alpha at 10 uM | 2006 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 16, Issue:18 | Synthesis, biochemical evaluation and rationalisation of the inhibitory activity of a range of 4-substituted phenyl alkyl imidazole-based inhibitors of the enzyme complex 17alpha-hydroxylase/17,20-lyase (P450(17alpha)). |
| AID1275144 | Antifungal activity against Candida tropicalis NRLL Y-12968 after 48 hrs by broth microdilution method | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Synthesis and biological evaluation of new naphthalene substituted thiosemicarbazone derivatives as potent antifungal and anticancer agents. |
| AID322155 | Antifungal activity against Candida albicans C 127-2000 after 48 hrs by CLSI M27-A2 method | 2008 | Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1 | N-Phenyl and N-phenylalkyl-maleimides acting against Candida spp.: time-to-kill, stability, interaction with maleamic acids. |
| AID524794 | Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay | 2009 | Nature chemical biology, Oct, Volume: 5, Issue:10 | Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum. |
| AID555817 | Antifungal activity against cdr2/cdr2 deficient Candida albicans STY7 after 48 hrs | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | Relative contributions of the Candida albicans ABC transporters Cdr1p and Cdr2p to clinical azole resistance. |
| AID387613 | Inhibition of human aromatase by fluorometric assay | 2008 | Bioorganic & medicinal chemistry, Sep-15, Volume: 16, Issue:18 | Screening of herbal constituents for aromatase inhibitory activity. |
| AID429608 | Inhibition of 17,20-lyase activity of rat testicular microsomal P450-17alpha | 2009 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 19, Issue:16 | Synthesis and biochemical evaluation of a range of sulfonated derivatives of 4-hydroxybenzyl imidazole as highly potent inhibitors of rat testicular 17alpha-hydroxylase/17,20-lyase (P-450(17alpha)). |
| AID594135 | Antimicrobial activity against Escherichia coli ATCC 25922 after 24 hrs by agar well diffusion method | 2011 | European journal of medicinal chemistry, May, Volume: 46, Issue:5 | Synthesis, antimicrobial, antioxidant, anti-hemolytic and cytotoxic evaluation of new imidazole-based heterocycles. |
| AID768392 | Antifungal activity against Aspergillus niger MTCC 282 by conventional broth microdilution method | 2013 | European journal of medicinal chemistry, Sep, Volume: 67 | Synthesis, antimicrobial and cytotoxic activities of some novel thiazole clubbed 1,3,4-oxadiazoles. |
| AID454773 | Antifungal activity against Candida albicans ATCC 10231 after 48 hrs by broth microdilution technique | 2009 | Bioorganic & medicinal chemistry, Nov-01, Volume: 17, Issue:21 | 5-Nitrofuranes and 5-nitrothiophenes with anti-Trypanosoma cruzi activity and ability to accumulate squalene. |
| AID420071 | Antifungal activity against Candida krusei after 48 hrs by broth microdilution assay | 2009 | Bioorganic & medicinal chemistry, Jun-01, Volume: 17, Issue:11 | Bulky 1,4-benzoxazine derivatives with antifungal activity. |
| AID510160 | Antifungal activity against Candida parapsilosis ATCC 22019 by spectrophotometry | 2010 | European journal of medicinal chemistry, Sep, Volume: 45, Issue:9 | A study of cytotoxicity of novel chlorokojic acid derivatives with their antimicrobial and antiviral activities. |
| AID287384 | Antifungal activity against Debaryomyces hansenii after 24 hrs by disk diffusion method | 2007 | European journal of medicinal chemistry, Feb, Volume: 42, Issue:2 | Synthesis, characterization and antimicrobial activity of Fe(II), Zn(II), Cd(II) and Hg(II) complexes with 2,6-bis(benzimidazol-2-yl) pyridine ligand. |
| AID1155878 | Cytotoxicity against human HCT15 cells assessed as growth inhibition at 50 uM after 48 hrs by SRB method | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Synthesis and cytotoxic effect on cancer cell lines and macrophages of novel progesterone derivatives having an ester or a carbamate function at C-3 and C-17. |
| AID1184071 | Inhibition of mouse TDO expressed in mouse P815B cells using L-tryptophan substrate incubated for 24 hrs by HPLC based cellular assay | 2014 | European journal of medicinal chemistry, Sep-12, Volume: 84 | Detailed analysis and follow-up studies of a high-throughput screening for indoleamine 2,3-dioxygenase 1 (IDO1) inhibitors. |
| AID283199 | Susceptibility of Candida glabrata 21231 isolate at 15 ug by disk diffusion method | 2007 | Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3 | Reduced susceptibility to polyenes associated with a missense mutation in the ERG6 gene in a clinical isolate of Candida glabrata with pseudohyphal growth. |
| AID481666 | Antifungal activity against Candida parapsilosis NRRL Y-12696 after 24 hrs by broth microdilution assay | 2010 | European journal of medicinal chemistry, May, Volume: 45, Issue:5 | Synthesis and the selective antifungal activity of 5,6,7,8-tetrahydroimidazo[1,2-a]pyridine derivatives. |
| AID47583 | Evaluation of In vitro antifungal activity against Candida albicans 76 by broth macro dilution method | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20 | Synthesis and antifungal activity of new azole derivatives containing an N-acylmorpholine ring. |
| AID1196740 | Antifungal activity against Aspergillus niger ATCC 1094 after 72 hrs by broth microdilution assay | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | A novel series of thiazolyl-pyrazoline derivatives: synthesis and evaluation of antifungal activity, cytotoxicity and genotoxicity. |
| AID551098 | Antifungal activity against Aspergillus niger by liquid dilution method | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1 | 3-[Benzimidazo- and 3-[benzothiadiazoleimidazo-(1,2-c)quinazolin-5-yl]-2H-chromene-2-ones as potent antimicrobial agents. |
| AID295127 | Antifungal activity against Rhodotorula rubra DSM 70403 at 20 ug after 72 hrs by disk diffusion method | 2007 | European journal of medicinal chemistry, Aug, Volume: 42, Issue:8 | Raman, FT-IR, NMR spectroscopic data and antimicrobial activity of bis[micro2-(benzimidazol-2-yl)-2-ethanethiolato-N,S,S-chloro-palladium(II)] dimer, [(micro2-CH2CH2NHNCC6H4)PdCl]2.C2H5OH complex. |
| AID1176153 | Inhibition of human recombinant CYP3A4 expressed in insect cell microsomes preincubated for 10 mins at 10 uM by fluorescence assay | 2015 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2 | Investigating the binding interactions of the anti-Alzheimer's drug donepezil with CYP3A4 and P-glycoprotein. |
| AID377674 | Antifungal activity against azole-resistant Candida albicans CN1A after 48 hrs by NCCLS M27A method | 2006 | Journal of natural products, Jul, Volume: 69, Issue:7 | Phytochemistry and antifungal properties of the newly discovered tree Pleodendron costaricense. |
| AID588211 | Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans | 2010 | Chemical research in toxicology, Jan, Volume: 23, Issue:1 | Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species. |
| AID575111 | Antifungal activity against Madurella mycetomatis isolate 46 by XTT assay | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Madurella mycetomatis is not susceptible to the echinocandin class of antifungal agents. |
| AID582799 | Antifungal activity against Candida albicans isolate 12 harboring ERG3 W332R mutant gene by broth microdilution method | 2010 | Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11 | Identification and characterization of four azole-resistant erg3 mutants of Candida albicans. |
| AID420663 | Antifungal activity against Candida tropicalis by micro-broth dilution method | 2009 | European journal of medicinal chemistry, May, Volume: 44, Issue:5 | Design, synthesis, and biological evaluation of novel triazole derivatives as inhibitors of cytochrome P450 14alpha-demethylase. |
| AID1130375 | Antifungal activity against Trichophyton mentagrophytes assessed as growth inhibition in sabouraud broth after 14 days | 1979 | Journal of medicinal chemistry, Aug, Volume: 22, Issue:8 | Antimycotic imidazoles. part 4. Synthesis and antifungal activity of ketoconazole, a new potent orally active broad-spectrum antifungal agent. |
| AID73608 | The compound was evaluated for mean zone diameter (inhibition) against filamentous fungi at 125 ug/mL concentration | 1987 | Journal of medicinal chemistry, Aug, Volume: 30, Issue:8 | Lysosomotropic agents. 7. Broad-spectrum antifungal activity of lysosomotropic detergents. |
| AID50141 | Evaluation of In vitro antifungal activity against Candida krusei C64 by broth macro dilution method | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20 | Synthesis and antifungal activity of new azole derivatives containing an N-acylmorpholine ring. |
| AID405025 | Antifungal activity against Sporothrix schenckii P14954 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by Sensititre YeastOne method | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods. |
| AID362910 | Antifungal activity against Aspergillus fumigatus after 24 hrs by broth microdilution method | 2008 | Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17 | NO-donors. Part 17: Synthesis and antimicrobial activity of novel ketoconazole-NO-donor hybrid compounds. |
| AID42874 | Inhibition of Candida krusei ATCC 6258 growth for 24 hours in vitro. | 2001 | Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17 | 3-Phenyl-5-acyloxymethyl-2H,5H-furan-2-ones: synthesis and biological activity of a novel group of potential antifungal drugs. |
| AID220095 | The compound was evaluated for mean zone diameter (inhibition) against yeast at the concentration of 250 ug/mL | 1987 | Journal of medicinal chemistry, Aug, Volume: 30, Issue:8 | Lysosomotropic agents. 7. Broad-spectrum antifungal activity of lysosomotropic detergents. |
| AID55176 | Minimum inhibitory concentration of compound for antifungal activity against Cryptococcus neoformans | 2000 | Bioorganic & medicinal chemistry letters, Oct-02, Volume: 10, Issue:19 | Novel antifungals based on 4-substituted imidazole: a combinatorial chemistry approach to lead discovery and optimization. |
| AID287715 | Antitrypanosomatid activity against Trypanosoma cruzi Y epimastigotes assessed as reduction of growth after 5 days | 2007 | Bioorganic & medicinal chemistry, Apr-01, Volume: 15, Issue:7 | Second generation of 5-ethenylbenzofuroxan derivatives as inhibitors of Trypanosoma cruzi growth: synthesis, biological evaluation, and structure-activity relationships. |
| AID262710 | Inhibition of human CYP17 expressed in Escherichia coli at 2.5 uM | 2006 | Journal of medicinal chemistry, Apr-06, Volume: 49, Issue:7 | Synthesis and evaluation of heteroaryl-substituted dihydronaphthalenes and indenes: potent and selective inhibitors of aldosterone synthase (CYP11B2) for the treatment of congestive heart failure and myocardial fibrosis. |
| AID343559 | Cytotoxicity against mouse J774 cells after 48 hrs by MTT assay | 2008 | Bioorganic & medicinal chemistry, Jul-15, Volume: 16, Issue:14 | New trypanocidal hybrid compounds from the association of hydrazone moieties and benzofuroxan heterocycle. |
| AID420073 | Antifungal activity against Candida glabrata after 48 hrs by broth microdilution assay | 2009 | Bioorganic & medicinal chemistry, Jun-01, Volume: 17, Issue:11 | Bulky 1,4-benzoxazine derivatives with antifungal activity. |
| AID644185 | Antifungal activity against Aspergillus flavus ATCC 9643 after 72 hrs by serial dilution method | 2012 | Bioorganic & medicinal chemistry, Feb-15, Volume: 20, Issue:4 | Synthesis of novel sulfonamide-1,2,4-triazoles, 1,3,4-thiadiazoles and 1,3,4-oxadiazoles, as potential antibacterial and antifungal agents. Biological evaluation and conformational analysis studies. |
| AID1209457 | Unbound Cmax in human plasma | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1 | In vitro inhibition of the bile salt export pump correlates with risk of cholestatic drug-induced liver injury in humans. |
| AID244975 | Minimum inhibitory concentration to inhibit Candida parapsilosis ATCC 22019 | 2004 | Journal of medicinal chemistry, Jul-29, Volume: 47, Issue:16 | Imidazole analogues of fluoxetine, a novel class of anti-Candida agents. |
| AID669127 | Antimicrobial activity against Malassezia pachydermatis infected in CD-1 mouse model of dandruff assessed as fungal hyphae fragmentation at 2% cream administered once daily for 6 days measured daily for 20 days | 2012 | Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7 | Molecular cloning, characterization, and inhibition studies of a β-carbonic anhydrase from Malassezia globosa, a potential antidandruff target. |
| AID363711 | Antifungal activity against Saccharomyces cerevisiae ATCC 9763 after 48 hrs by broth microdilution technique | 2008 | Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17 | In vitro antifungal activity of polyfunctionalized 2-(hetero)arylquinolines prepared through imino Diels-Alder reactions. |
| AID53566 | Inhibition of cytochrome P450 19A1 involved in steroid biosynthesis | 1992 | Journal of medicinal chemistry, Jul-24, Volume: 35, Issue:15 | Stereoisomers of ketoconazole: preparation and biological activity. |
| AID481671 | Cytotoxicity against human SKOV3 cells up to 25 ug/ml after 48 hrs by neutral red assay | 2010 | European journal of medicinal chemistry, May, Volume: 45, Issue:5 | Synthesis and the selective antifungal activity of 5,6,7,8-tetrahydroimidazo[1,2-a]pyridine derivatives. |
| AID340959 | Antifungal activity against Candida parapsilosis ATCC 22013 by NCCLS M27-A2 method | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8 | Cross-resistance to medical and agricultural azole drugs in yeasts from the oropharynx of human immunodeficiency virus patients and from environmental Bavarian vine grapes. |
| AID47587 | Evaluation of In vivo antifungal activity against Candida albicans 60 by broth macro dilution method | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20 | Synthesis and antifungal activity of new azole derivatives containing an N-acylmorpholine ring. |
| AID681142 | TP_TRANSPORTER: increase in Vinblastine intracellular accumulation in MDR1-expressing LLC-PK1 cells | 2002 | Molecular pharmacology, May, Volume: 61, Issue:5 | Three-dimensional quantitative structure-activity relationships of inhibitors of P-glycoprotein. |
| AID303382 | Selectivity index, ratio of IC50 for human THP1 cells to IC50 for Trypanosoma cruzi Tulahuen 2 | 2007 | Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24 | In vivo anti-Chagas vinylthio-, vinylsulfinyl-, and vinylsulfonylbenzofuroxan derivatives. |
| AID405096 | Antimicrobial activity against Mucor sp. after 24 hrs | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | In vitro susceptibilities of 217 clinical isolates of zygomycetes to conventional and new antifungal agents. |
| AID533801 | Antifungal activity against Cryptococcus neoformans ATCC 32264 by agar dilution method | 2010 | European journal of medicinal chemistry, Nov, Volume: 45, Issue:11 | Synthesis and biological evaluation of N-antipyrine-4-substituted amino-3-chloromaleimide derivatives. |
| AID463408 | Antimicrobial activity against Aspergillus niger at 1000 ug after 72 hrs by cup plate method | 2010 | European journal of medicinal chemistry, Mar, Volume: 45, Issue:3 | Antimicrobial study of newly synthesized 6-substituted indolo[1,2-c]quinazolines. |
| AID531189 | Antifungal activity against Trichophyton rubrum ATCC MYA-4438 at 9.4 uM after 5 days by CLSI method | 2008 | Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7 | Potent in vitro antifungal activities of naturally occurring acetylenic acids. |
| AID244039 | In vitro inhibition of human CYP11B2 expressed in Schizosaccharomyces pombe incubated with 100 nM of substrate deoxy-corticosterone in presence of 500 nM of compound | 2005 | Journal of medicinal chemistry, Mar-10, Volume: 48, Issue:5 | Synthesis and evaluation of (pyridylmethylene)tetrahydronaphthalenes/-indanes and structurally modified derivatives: potent and selective inhibitors of aldosterone synthase. |
| AID977602 | Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM | 2013 | Molecular pharmacology, Jun, Volume: 83, Issue:6 | Structure-based identification of OATP1B1/3 inhibitors. |
| AID1216149 | Inhibition of human recombinant CYP4F2 assessed as fingolimod metabolism | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2 | CYP4F enzymes are responsible for the elimination of fingolimod (FTY720), a novel treatment of relapsing multiple sclerosis. |
| AID415955 | Antimicrobial activity against Aspergillus fumigatus by micro-broth dilution method | 2009 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6 | Design, synthesis, and biological evaluation of novel 1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluorophenyl)-3-substituted benzylamino-2-propanols. |
| AID48820 | The compound was tested for antifungal activity against Candida tropicalis MY1011 using agar dilution assay | 1987 | Journal of medicinal chemistry, Aug, Volume: 30, Issue:8 | Lysosomotropic agents. 7. Broad-spectrum antifungal activity of lysosomotropic detergents. |
| AID574265 | Antifungal activity against 48 hrs cultures of 10'7 cells/ml Candida albicans ATCC 90028 biofilms by XTT reduction method | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | Cell density and cell aging as factors modulating antifungal resistance of Candida albicans biofilms. |
| AID255080 | Inhibitory concentration against human cytochrome P450 11B1 expressed in fission yeast, incubated with [14C]deoxycorticosterone | 2005 | Journal of medicinal chemistry, Oct-20, Volume: 48, Issue:21 | Heteroaryl-substituted naphthalenes and structurally modified derivatives: selective inhibitors of CYP11B2 for the treatment of congestive heart failure and myocardial fibrosis. |
| AID53211 | Evaluated for the inhibitory activity towards Cytochrome P450 17 human enzyme using testicular microsome at 25 uM of substrate (progesterone) | 2000 | Journal of medicinal chemistry, Nov-02, Volume: 43, Issue:22 | Synthesis and evaluation of novel steroidal oxime inhibitors of P450 17 (17 alpha-hydroxylase/C17-20-lyase) and 5 alpha-reductase types 1 and 2. |
| AID323060 | Antifungal activity against Cryptococcus neoformans ATCC 32264 by microbroth dilution method | 2008 | Bioorganic & medicinal chemistry, Jan-15, Volume: 16, Issue:2 | Antifungal and cytotoxic activities of some N-substituted aniline derivatives bearing a hetaryl fragment. |
| AID696541 | Antifungal activity against Aspergillus flavus ATCC 9170 after 48 hrs by broth microdilution technique | 2012 | Bioorganic & medicinal chemistry, Nov-01, Volume: 20, Issue:21 | Synthesis and antifungal activity of diverse C-2 pyridinyl and pyridinylvinyl substituted quinolines. |
| AID554725 | Fold resistant, ratio of MIC for Saccharomyces cerevisiae isolate ADdelta overexpressing Candida krusei ERG11g to MIC for Saccharomyces cerevisiae isolate ADdelta overexpressing Abc1p | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2 | Abc1p is a multidrug efflux transporter that tips the balance in favor of innate azole resistance in Candida krusei. |
| AID625289 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID1265640 | Antifungal activity against Candida albicans clinical isolate after 24 hrs by sabouraud dextrose broth based microdilution method | 2016 | European journal of medicinal chemistry, Jan-01, Volume: 107 | Anti-Candida activity and cytotoxicity of a large library of new N-substituted-1,3-thiazolidin-4-one derivatives. |
| AID2948 | Percent inhibition of 17-alpha-hydroxylase/17,20 lyase of rat testes microsomes at 100 uM | 1990 | Journal of medicinal chemistry, Sep, Volume: 33, Issue:9 | Hydroxyperfluoroazobenzenes: novel inhibitors of enzymes of androgen biosynthesis. |
| AID323065 | Antifungal activity against Trichophyton rubrum C113 by microbroth dilution method | 2008 | Bioorganic & medicinal chemistry, Jan-15, Volume: 16, Issue:2 | Antifungal and cytotoxic activities of some N-substituted aniline derivatives bearing a hetaryl fragment. |
| AID363769 | Antimicrobial activity against Candida krusei C117 isolate at 6.25 ug/ml after 24 hrs | 2008 | Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17 | In vitro antifungal activity of polyfunctionalized 2-(hetero)arylquinolines prepared through imino Diels-Alder reactions. |
| AID600772 | Antifungal activity against Fusarium sporotrichioides IMT 496 after 72 hrs by serial dilution method | 2011 | Bioorganic & medicinal chemistry, May-15, Volume: 19, Issue:10 | Thiazole-based chalcones as potent antimicrobial agents. Synthesis and biological evaluation. |
| AID616876 | Antimicrobial activity against Candida albicans after 24 hrs by agar dilution method | 2011 | Journal of natural products, Aug-26, Volume: 74, Issue:8 | Cytotoxic bipyridines from the marine-derived actinomycete Actinoalloteichus cyanogriseus WH1-2216-6. |
| AID1238922 | Antifungal activity against Candida glabrata ATCC 90030 WTBF-86 by microbroth dilution method | 2015 | Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17 | Synthesis and antifungal evaluation of head-to-head and head-to-tail bisamidine compounds. |
| AID48615 | Evaluation of In vitro antifungal activity against Candida tropicalis 50 by broth macro dilution method | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20 | Synthesis and antifungal activity of new azole derivatives containing an N-acylmorpholine ring. |
| AID599147 | Antibacterial activity against Escherichia coli after 24 hrs by MTT assay | 2008 | European journal of medicinal chemistry, Mar, Volume: 43, Issue:3 | Synthesis, crystal structure and antimicrobial activity of deoxybenzoin derivatives from genistein. |
| AID477746 | Antimicrobial activity against Aspergillus fumigatus after 24 hrs | 2010 | European journal of medicinal chemistry, Apr, Volume: 45, Issue:4 | An eco-friendly synthesis and antimicrobial activities of dihydro-2H-benzo- and naphtho-1,3-oxazine derivatives. |
| AID1222388 | Inhibition of human recombinant UGT1A1 expressed in HEK293 cells assessed as reduction in bilirubin glucuronidation by LC-MS/MS method | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2 | Correlation between bilirubin glucuronidation and estradiol-3-gluronidation in the presence of model UDP-glucuronosyltransferase 1A1 substrates/inhibitors. |
| AID322153 | Antifungal activity against Candida albicans C 125-2000 after 48 hrs by CLSI M27-A2 method | 2008 | Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1 | N-Phenyl and N-phenylalkyl-maleimides acting against Candida spp.: time-to-kill, stability, interaction with maleamic acids. |
| AID1247098 | Antifungal activity against Candida albicans after 48 to 72 hrs by two fold serial dilution method | 2015 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19 | Synthesis of BF₃ catalyzed Mannich derivatives with excellent ee from phenylpropanolamine, study of their antimicrobial activity and molecular docking. |
| AID429610 | Selectivity index, ratio of IC50 for 17-alpha-hydroxylase activity of rat testicular microsomal P450-17alpha to IC50 for 17,20-lyase activity of rat testicular microsomal P450-17alpha | 2009 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 19, Issue:16 | Synthesis and biochemical evaluation of a range of sulfonated derivatives of 4-hydroxybenzyl imidazole as highly potent inhibitors of rat testicular 17alpha-hydroxylase/17,20-lyase (P-450(17alpha)). |
| AID1079942 | Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source] | |||
| AID481914 | Antifungal activity against Candida tropicalis ATCC 12968 at 15 ug in 6 mm disk after 10 hrs by disc-diffusion assay | 2010 | Journal of natural products, May-28, Volume: 73, Issue:5 | Chemical epigenetics alters the secondary metabolite composition of guttate excreted by an atlantic-forest-soil-derived Penicillium citreonigrum. |
| AID1067045 | Antifungal activity against Aspergillus fumigatus by micro-broth dilution method | 2014 | European journal of medicinal chemistry, Mar-03, Volume: 74 | Synthesis, antifungal activities and molecular docking studies of novel 2-(2,4-difluorophenyl)-2-hydroxy-3-(1H-1,2,4-triazol-1-yl)propyl dithiocarbamates. |
| AID554715 | Antimicrobial activity against Candida krusei NZCDC 89.221 after 48 hrs by CLSI method | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2 | Abc1p is a multidrug efflux transporter that tips the balance in favor of innate azole resistance in Candida krusei. |
| AID243960 | In vitro inhibition of human cytochrome P450 11B2 expressed in Schizosaccharomyces pombe with 500 nM deoxy-corticosterone; nd= not determined | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Synthesis and evaluation of imidazolylmethylenetetrahydronaphthalenes and imidazolylmethyleneindanes: potent inhibitors of aldosterone synthase. |
| AID425723 | Antimicrobial activity against Balamuthia mandrillaris ATCC 50209 infected in HBMEC assessed as inhibition of amoeba-induced cytopathogenicity at 10 ug/mL after 24 hrs by LDH release assay | 2007 | Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12 | Effect of antimicrobial compounds on Balamuthia mandrillaris encystment and human brain microvascular endothelial cell cytopathogenicity. |
| AID600767 | Antifungal activity against Aspergillus niger ATCC 6275 after 72 hrs by serial dilution method | 2011 | Bioorganic & medicinal chemistry, May-15, Volume: 19, Issue:10 | Thiazole-based chalcones as potent antimicrobial agents. Synthesis and biological evaluation. |
| AID644195 | Antifungal activity against Fulvia fulva treated for 72 hrs followed by sub-cultivated for 5 days by serial dilution method | 2012 | Bioorganic & medicinal chemistry, Feb-15, Volume: 20, Issue:4 | Synthesis of novel sulfonamide-1,2,4-triazoles, 1,3,4-thiadiazoles and 1,3,4-oxadiazoles, as potential antibacterial and antifungal agents. Biological evaluation and conformational analysis studies. |
| AID633953 | Antifungal activity against Aspergillus flavus ATCC 9643 after 72 hrs by serial dilution technique | 2011 | Bioorganic & medicinal chemistry, Dec-15, Volume: 19, Issue:24 | Novel (E)-1-(4-methyl-2-(alkylamino)thiazol-5-yl)-3-arylprop-2-en-1-ones as potent antimicrobial agents. |
| AID633960 | Antifungal activity against Aspergillus niger ATCC 6275 incubated for 72 hrs followed by serial sub-cultivation for 72 hrs by serial dilution technique | 2011 | Bioorganic & medicinal chemistry, Dec-15, Volume: 19, Issue:24 | Novel (E)-1-(4-methyl-2-(alkylamino)thiazol-5-yl)-3-arylprop-2-en-1-ones as potent antimicrobial agents. |
| AID502081 | Inhibition of 17-alpha-hydroxylase activity of rat testicular microsomal P450-17alpha | 2010 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 20, Issue:17 | Synthesis and biochemical evaluation of a range of (4-substituted phenyl)sulfonate derivatives of 4-hydroxybenzyl imidazole-based compounds as potent inhibitors of 17alpha-hydroxylase/17,20-lyase (P45017alpha) derived from rat testicular microsomes. |
| AID524790 | Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay | 2009 | Nature chemical biology, Oct, Volume: 5, Issue:10 | Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum. |
| AID208366 | In vitro Minimum lethal concentration was determined by microbroth dilution assay on Torulopsis glabrata | 1992 | Journal of medicinal chemistry, Jan, Volume: 35, Issue:1 | Synthesis, specificity, and antifungal activity of inhibitors of the Candida albicans delta 24-sterol methyltransferase. |
| AID1451792 | Antifungal activity against Trichophyton rubrum after 7 days | 2017 | Journal of medicinal chemistry, 10-12, Volume: 60, Issue:19 | Novel Inhibitors of Staphyloxanthin Virulence Factor in Comparison with Linezolid and Vancomycin versus Methicillin-Resistant, Linezolid-Resistant, and Vancomycin-Intermediate Staphylococcus aureus Infections in Vivo. |
| AID572693 | Binding affinity to Mycobacterium smegmatis ATCC 700084 CYP51 in presence of 0.5 M NaCl at pH7.5 | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | Identification, characterization, and azole-binding properties of Mycobacterium smegmatis CYP164A2, a homolog of ML2088, the sole cytochrome P450 gene of Mycobacterium leprae. |
| AID47586 | Evaluation of In vitro antifungal activity against Candida albicans C56 by broth macro dilution method | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20 | Synthesis and antifungal activity of new azole derivatives containing an N-acylmorpholine ring. |
| AID1176151 | Inhibition of human recombinant CYP3A4 expressed in insect cell microsomes preincubated for 10 mins at 0.1 uM by fluorescence assay | 2015 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2 | Investigating the binding interactions of the anti-Alzheimer's drug donepezil with CYP3A4 and P-glycoprotein. |
| AID515009 | Antifungal activity against Candida albicans Y0109 after 24 hrs by micro-broth dilution method | 2010 | European journal of medicinal chemistry, Oct, Volume: 45, Issue:10 | Synthesis and antifungal evaluation of novel triazole derivatives as inhibitors of cytochrome P450 14alpha-demethylase. |
| AID574262 | Antifungal activity against 48 hrs cultures of 10'7 cells/ml Candida albicans BF-1 planktonic cells by XTT reduction method | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | Cell density and cell aging as factors modulating antifungal resistance of Candida albicans biofilms. |
| AID405101 | Antimicrobial activity against Cunninghamella sp. after 24 hrs | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | In vitro susceptibilities of 217 clinical isolates of zygomycetes to conventional and new antifungal agents. |
| AID45331 | Evaluation of In vivo antifungal activity against Candida albicans 60 by broth macro dilution method | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20 | Synthesis and antifungal activity of new azole derivatives containing an N-acylmorpholine ring. |
| AID456681 | Antifungal activity against Cryptococcus neoformans ATCC 32264 assessed as inhibition of fungal growth at 200 uM after 48 hrs by microbroth dilution method | 2010 | Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1 | New small-size peptides possessing antifungal activity. |
| AID363964 | Antimicrobial activity against Cryptococcus neoformans IM 031706 isolate at 6.25 ug/ml after 48 hrs | 2008 | Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17 | In vitro antifungal activity of polyfunctionalized 2-(hetero)arylquinolines prepared through imino Diels-Alder reactions. |
| AID590622 | Antifungal activity against Curvularia lunata assessed as zone of inhibition at 100 ug/ml after 48 hrs by disc diffusion method | 2011 | European journal of medicinal chemistry, Apr, Volume: 46, Issue:4 | Synthesis and biological activity of 2-(bis((1,3,4-oxadiazolyl/1,3,4-thiadiazolyl)methylthio)methylene)malononitriles. |
| AID407004 | Antimicrobial activity against Candida albicans FH1 at planktonic cell density of 10'8 cells/ml after 48 hrs by XTT assay | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | Role for cell density in antifungal drug resistance in Candida albicans biofilms. |
| AID603181 | Antifungal activity against Candida albicans ATCC 10231 at 20 ug/ml after 24 hrs by cup plate method | 2011 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 21, Issue:13 | Practical synthesis, anticonvulsant, and antimicrobial activity of N-allyl and N-propargyl di(indolyl)indolin-2-ones. |
| AID330518 | Toxicity against human HepG2 cells at 100 ug/ml | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Mar-13, Volume: 104, Issue:11 | High-throughput synergy screening identifies microbial metabolites as combination agents for the treatment of fungal infections. |
| AID723702 | Fungicidal activity against Aspergillus fumigatus after 72 hrs by serial subcultivation method | 2013 | Bioorganic & medicinal chemistry, Jan-15, Volume: 21, Issue:2 | Synthesis and biological evaluation of some 5-arylidene-2-(1,3-thiazol-2-ylimino)-1,3-thiazolidin-4-ones as dual anti-inflammatory/antimicrobial agents. |
| AID39708 | In vitro minimum inhibitory concentration of compound was determined against Aspergillus fumigatus after 24 hr r | 2000 | Bioorganic & medicinal chemistry letters, Aug-21, Volume: 10, Issue:16 | 3-Phenyl-5-methyl-2H,5H-furan-2-ones: tuning antifungal activity by varying substituents on the phenyl ring. |
| AID491003 | Antifungal activity against Aspergillus niger after 48 hrs by microdilution susceptibility assay | 2010 | European journal of medicinal chemistry, Jul, Volume: 45, Issue:7 | Synthesis and bioassay of pyrrolyl oxazolines and thiazolines. |
| AID50294 | In vitro minimum inhibitory concentration of compound was determined against Candida krusei after 48 hr | 2000 | Bioorganic & medicinal chemistry letters, Aug-21, Volume: 10, Issue:16 | 3-Phenyl-5-methyl-2H,5H-furan-2-ones: tuning antifungal activity by varying substituents on the phenyl ring. |
| AID208365 | In vitro Minimum inhibitory concentration was determined by microbroth dilution assay on Torulopsis glabrata | 1992 | Journal of medicinal chemistry, Jan, Volume: 35, Issue:1 | Synthesis, specificity, and antifungal activity of inhibitors of the Candida albicans delta 24-sterol methyltransferase. |
| AID532572 | Antifungal activity against wild-type Candida glabrata isolate 21231 by disk diffusion method | 2008 | Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10 | A nonsense mutation in the ERG6 gene leads to reduced susceptibility to polyenes in a clinical isolate of Candida glabrata. |
| AID667062 | Antifungal activity against Penicillium chrysogenum after 48 hrs by broth dilution method | 2012 | European journal of medicinal chemistry, Aug, Volume: 54 | Synthesis, antimicrobial and cytotoxic activities of sulfone linked bis heterocycles. |
| AID315664 | Inhibition of recombinant CYP2B6 at 10 uM | 2008 | Bioorganic & medicinal chemistry, Feb-15, Volume: 16, Issue:4 | Synthesis, biological evaluation and molecular modelling studies of methyleneimidazole substituted biaryls as inhibitors of human 17alpha-hydroxylase-17,20-lyase (CYP17). Part I: Heterocyclic modifications of the core structure. |
| AID564269 | Antifungal activity against Candida albicans isolate 6 after 48 hrs by broth microdilution method | 2010 | Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9 | A clinical isolate of Candida albicans with mutations in ERG11 (encoding sterol 14alpha-demethylase) and ERG5 (encoding C22 desaturase) is cross resistant to azoles and amphotericin B. |
| AID553065 | Inhibition of human CYP11B1 expressed in hamster V79MZ cells using 11-deoxycorticosterone substrate | 2011 | ACS medicinal chemistry letters, Jan-13, Volume: 2, Issue:1 | First Selective CYP11B1 Inhibitors for the Treatment of Cortisol-Dependent Diseases. |
| AID77236 | In vivo inhibition in guinea pig trichophytosis model | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | Synthesis and structure-activity relationships of phenyl-substituted benzylamine antimycotics: a novel benzylbenzylamine antifungal agent for systemic treatment. |
| AID575114 | Antifungal activity against Madurella mycetomatis isolate 52 by XTT assay | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Madurella mycetomatis is not susceptible to the echinocandin class of antifungal agents. |
| AID636995 | Antifungal activity against Aspergillus fumigatus at 100 ug/disc after 24 hrs by disc diffusion method | 2012 | European journal of medicinal chemistry, Feb, Volume: 48 | Synthesis and biological evaluation of some thiazolidinones as antimicrobial agents. |
| AID1300882 | Antifungal activity against Candida parapsilosis clinical isolate after 24 hrs by broth microdilution method | 2016 | European journal of medicinal chemistry, Jul-19, Volume: 117 | Novel 1,3-thiazolidin-4-one derivatives as promising anti-Candida agents endowed with anti-oxidant and chelating properties. |
| AID1061002 | Antimicrobial activity against Aspergillus niger CGMCC3.316 after 48 hrs by twofold serial microdilution method | 2014 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1 | Synthesis and biological evaluation of novel N-substituted 1H-dibenzo[a,c]carbazole derivatives of dehydroabietic acid as potential antimicrobial agents. |
| AID625292 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID667054 | Antifungal activity against Aspergillus niger at 100 ug/ml after 48 hrs by agar well diffusion method | 2012 | European journal of medicinal chemistry, Aug, Volume: 54 | Synthesis, antimicrobial and cytotoxic activities of sulfone linked bis heterocycles. |
| AID690959 | Antifungal activity against Penicillium chrysogenum NCIM 738 after 48 hrs by NCCLS agar well diffusion method | 2012 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20 | Synthesis, characterization and biological evaluation of some novel 2,4-thiazolidinediones as potential cytotoxic, antimicrobial and antihyperglycemic agents. |
| AID48252 | 50% inhibitory activity against the Candida. species (40 clinical isolates) was determined at pH-7.2 | 1995 | Journal of medicinal chemistry, Oct-13, Volume: 38, Issue:21 | Antifungal agents. 9. 3-Aryl-4-[alpha-(1H-imidazol-1-yl)arylmethyl]pyrroles: a new class of potent anti-Candida agents. |
| AID634081 | Fungistatic activity against Saccharomyces cerevisiae ATCC 24657 assessed as cell proliferation compound after 24 to 48 hrs by agar plate bioassay | 2012 | European journal of medicinal chemistry, Jan, Volume: 47, Issue:1 | Antifungal activities of novel non-azole molecules against S. cerevisiae and C. albicans. |
| AID395651 | Antifungal activity against Cryptococcus neoformans ATCC 32264 assessed as growth inhibition at 200 uM after 48 hrs | 2009 | European journal of medicinal chemistry, Jan, Volume: 44, Issue:1 | Penetratin and derivatives acting as antifungal agents. |
| AID48432 | Tested In vitro for antifungal activity against candida Spp (Candida glabrata, Candida krusei) at pH 7.2 | 2002 | Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13 | Antifungal agents. 10. New derivatives of 1-[(aryl)[4-aryl-1H-pyrrol-3-yl]methyl]-1H-imidazole, synthesis, anti-candida activity, and quantitative structure-analysis relationship studies. |
| AID406953 | Cytotoxicity against human U937 cells assessed as reduction of cell viability after 24 hrs by MTT assay | 2008 | Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13 | 1-[(3-Aryloxy-3-aryl)propyl]-1H-imidazoles, new imidazoles with potent activity against Candida albicans and dermatophytes. Synthesis, structure-activity relationship, and molecular modeling studies. |
| AID391498 | Antifungal activity against Aspergillus flavus ATCC 9170 after 48 hrs by spectrophotometry | 2008 | Journal of natural products, Oct, Volume: 71, Issue:10 | Evidence for the mechanism of action of the antifungal phytolaccoside B isolated from Phytolacca tetramera Hauman. |
| AID448514 | Antimicrobial activity against Aspergillus niger at 30 ug/mL after 16 to 20 hrs by disk diffusion method | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11 | Synthesis of some novel pyrazolo[3,4-b]pyridine and pyrazolo[3,4-d]pyrimidine derivatives bearing 5,6-diphenyl-1,2,4-triazine moiety as potential antimicrobial agents. |
| AID269149 | Inhibition of rat microsomal 17,20-lyase component of P450-17alpha | 2006 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 16, Issue:15 | Synthesis and biochemical evaluation of a range of potent benzyl imidazole-based compounds as potential inhibitors of the enzyme complex 17alpha-hydroxylase/17,20-lyase (P450(17alpha)). |
| AID533804 | Antifungal activity against Trichophyton mentagrophytes ATCC 9972 by agar dilution method | 2010 | European journal of medicinal chemistry, Nov, Volume: 45, Issue:11 | Synthesis and biological evaluation of N-antipyrine-4-substituted amino-3-chloromaleimide derivatives. |
| AID405099 | Antimicrobial activity against Rhizomucor sp. after 24 hrs | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | In vitro susceptibilities of 217 clinical isolates of zygomycetes to conventional and new antifungal agents. |
| AID648371 | Antifungal activity against Candida albicans MTCC 227 at 1000 ug/disc after 48 hrs by disc diffusion assay | 2012 | European journal of medicinal chemistry, May, Volume: 51 | Synthesis of novel spirooxindole derivatives by one pot multicomponent reaction and their antimicrobial activity. |
| AID1067044 | Antifungal activity against Candida glabrata by micro-broth dilution method | 2014 | European journal of medicinal chemistry, Mar-03, Volume: 74 | Synthesis, antifungal activities and molecular docking studies of novel 2-(2,4-difluorophenyl)-2-hydroxy-3-(1H-1,2,4-triazol-1-yl)propyl dithiocarbamates. |
| AID690958 | Antifungal activity against Aspergillus oryzae NCIM 643 after 48 hrs by NCCLS agar well diffusion method | 2012 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20 | Synthesis, characterization and biological evaluation of some novel 2,4-thiazolidinediones as potential cytotoxic, antimicrobial and antihyperglycemic agents. |
| AID406859 | Antimicrobial activity against Candida albicans SC5314 at planktonic cell density of 10'8 cells/ml after 48 hrs by XTT assay | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | Role for cell density in antifungal drug resistance in Candida albicans biofilms. |
| AID42876 | Inhibition of Candida krusei E28 growth for 24 hours in vitro. | 2001 | Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17 | 3-Phenyl-5-acyloxymethyl-2H,5H-furan-2-ones: synthesis and biological activity of a novel group of potential antifungal drugs. |
| AID1176935 | Antimicrobial activity against Candida albicans CGMCC2.2086 after 48 hrs by modified microdilution method | 2015 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3 | Synthesis, in vitro antimicrobial and cytotoxic activities of new carbazole derivatives of ursolic acid. |
| AID1210015 | Inhibition of CYP1A2 in human liver microsomes using phenacetin as substrate after 8 mins by LC-MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5 | Identifying a selective substrate and inhibitor pair for the evaluation of CYP2J2 activity. |
| AID53373 | Tested for inhibition of human testicular C17,20-Lyase. | 1995 | Journal of medicinal chemistry, Oct-13, Volume: 38, Issue:21 | Esters of 3-pyridylacetic acid that combine potent inhibition of 17 alpha-hydroxylase/C17,20-lyase (cytochrome P45017 alpha) with resistance to esterase hydrolysis. |
| AID1223624 | Inhibition of CYP3A4 activity in human liver microsomes using testosterone as a substrate by LC/MS analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4 | Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID377677 | Antifungal activity against Saccharomyces cerevisiae after 48 hrs by NCCLS M27A method | 2006 | Journal of natural products, Jul, Volume: 69, Issue:7 | Phytochemistry and antifungal properties of the newly discovered tree Pleodendron costaricense. |
| AID481912 | Antifungal activity against Candida parapsilosis ATCC 12969 at 15 ug in 6 mm disk after 10 hrs by disc-diffusion assay | 2010 | Journal of natural products, May-28, Volume: 73, Issue:5 | Chemical epigenetics alters the secondary metabolite composition of guttate excreted by an atlantic-forest-soil-derived Penicillium citreonigrum. |
| AID51626 | Inhibition of cytochrome P450 Cholesterol 7-alpha-hydroxylase | 1992 | Journal of medicinal chemistry, Jul-24, Volume: 35, Issue:15 | Stereoisomers of ketoconazole: preparation and biological activity. |
| AID596446 | Antifungal activity against Cryptococcus neoformans ATCC 32264 | 2011 | Bioorganic & medicinal chemistry, May-01, Volume: 19, Issue:9 | Antifungal, cytotoxic and SAR studies of a series of N-alkyl, N-aryl and N-alkylphenyl-1,4-pyrrolediones and related compounds. |
| AID295131 | Antifungal activity against Debaryomyces hansenii DSM 70238 at 20 ug after 72 hrs by disk diffusion method | 2007 | European journal of medicinal chemistry, Aug, Volume: 42, Issue:8 | Raman, FT-IR, NMR spectroscopic data and antimicrobial activity of bis[micro2-(benzimidazol-2-yl)-2-ethanethiolato-N,S,S-chloro-palladium(II)] dimer, [(micro2-CH2CH2NHNCC6H4)PdCl]2.C2H5OH complex. |
| AID313556 | Inhibition of hepatic CYP3A4 at 10 uM | 2008 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 18, Issue:1 | Synthesis, biological evaluation and molecular modelling studies of novel ACD- and ABD-ring steroidomimetics as inhibitors of CYP17. |
| AID362166 | Inhibition of human CYP11B2 expressed in hamster V79MZh11B2 cells | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16 | Synthesis, biological evaluation, and molecular modeling of abiraterone analogues: novel CYP17 inhibitors for the treatment of prostate cancer. |
| AID214846 | Percent Inhibition of growth of uM | 2002 | Journal of medicinal chemistry, Aug-29, Volume: 45, Issue:18 | Design, synthesis, and biological evaluation of aryloxyethyl thiocyanate derivatives against Trypanosoma cruzi. |
| AID405102 | Antimicrobial activity against Apophysomyces elegans after 24 hrs | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | In vitro susceptibilities of 217 clinical isolates of zygomycetes to conventional and new antifungal agents. |
| AID667055 | Antifungal activity against Penicillium chrysogenum at 50 ug/ml after 48 hrs by agar well diffusion method | 2012 | European journal of medicinal chemistry, Aug, Volume: 54 | Synthesis, antimicrobial and cytotoxic activities of sulfone linked bis heterocycles. |
| AID367168 | Cytotoxicity against human A431 cells at 1 mg/ml | 2009 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 19, Issue:3 | Synthesis and antifungal activity of 1,2,3-triazole containing fluconazole analogues. |
| AID1319259 | Inhibition of CYP3A4 in human liver microsomes using midazolam as substrate assessed as reduction in 1-OH-midazolam formation at 0.02 uM by LC/MS/MS analysis | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18 | Identification of (R)-(2-Chloro-3-(trifluoromethyl)phenyl)(1-(5-fluoropyridin-2-yl)-4-methyl-6,7-dihydro-1H-imidazo[4,5-c]pyridin-5(4H)-yl)methanone (JNJ 54166060), a Small Molecule Antagonist of the P2X7 receptor. |
| AID315656 | Inhibition of recombinant CYP3A4 at 10 uM | 2008 | Bioorganic & medicinal chemistry, Feb-15, Volume: 16, Issue:4 | Synthesis, biological evaluation and molecular modelling studies of methyleneimidazole substituted biaryls as inhibitors of human 17alpha-hydroxylase-17,20-lyase (CYP17). Part I: Heterocyclic modifications of the core structure. |
| AID488644 | Antimicrobial activity against Candida dubliniensis ATCC 778157 by broth dilution method | 2010 | Journal of natural products, Jun-25, Volume: 73, Issue:6 | Alkaloids from the bark of Guatteria hispida and their evaluation as antioxidant and antimicrobial agents. |
| AID214432 | In vitro antifungal activity against Trichophyton schoenleinii ATCC 22775 | 1988 | Journal of medicinal chemistry, Oct, Volume: 31, Issue:10 | Studies on antifungal agents. 23. Novel substituted 3,5-diphenyl-3-(1H-imidazol-1-ylmethyl)- 2-alkylisoxazolidine derivatives. |
| AID348156 | Selectivity index, ratio of IC50 for mouse J774 cells to IC50 for Trypanosoma cruzi Tulahuen 2 | 2009 | Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2 | Synthesis, trypanocidal activity and docking studies of novel quinoxaline-N-acylhydrazones, designed as cruzain inhibitors candidates. |
| AID574252 | Antifungal activity against 24 hrs cultures of 10'7 cells/ml Candida albicans ATCC 90028 biofilms by XTT reduction assay | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | Cell density and cell aging as factors modulating antifungal resistance of Candida albicans biofilms. |
| AID494006 | Antifungal activity against Cryptococcus neoformans ATCC 32264 assessed as inhibition of fungal growth at 25 uM | 2010 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 20, Issue:16 | New antifungal peptides. Synthesis, bioassays and initial structure prediction by CD spectroscopy. |
| AID1057770 | Antimicrobial activity against Candida glabrata ATCC 90030 after 24 hrs by broth microdilution method | 2013 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24 | Synthesis and initial biological evaluation of substituted 1-phenylamino-2-thio-4,5-dimethyl-1H-imidazole derivatives. |
| AID688637 | Antifungal activity against Penicillium chrysogenum at 100 ug after 48 hrs by agar well diffusion method | 2011 | European journal of medicinal chemistry, Nov, Volume: 46, Issue:11 | Synthesis and antimicrobial activity of amido linked pyrrolyl and pyrazolyl-oxazoles, thiazoles and imidazoles. |
| AID376045 | Antifungal activity against Microsporum gypseum C 115 by agar dilution method | 1999 | Journal of natural products, Oct, Volume: 62, Issue:10 | In vitro evaluation of antifungal properties of phenylpropanoids and related compounds acting against dermatophytes. |
| AID376046 | Antifungal activity against Trichophyton mentagrophytes ATCC by agar dilution method | 1999 | Journal of natural products, Oct, Volume: 62, Issue:10 | In vitro evaluation of antifungal properties of phenylpropanoids and related compounds acting against dermatophytes. |
| AID633910 | Antifungal activity against Candida albicans ATCC 90028 at 10 ug/mL after 72 hrs by agar cup plate method | 2012 | European journal of medicinal chemistry, Jan, Volume: 47, Issue:1 | Isoxazoles incorporated N-substituted decahydroquinolines: a precursor to the next generation antimicrobial drug. |
| AID287723 | Inhibition of human recombinant aromatase at 10 uM after 30 mins relative to control | 2007 | Bioorganic & medicinal chemistry, Apr-01, Volume: 15, Issue:7 | Synthesis of DL-standishinal and its related compounds for the studies on structure-activity relationship of inhibitory activity against aromatase. |
| AID47865 | Evaluation of In vitro antifungal activity against Candida parapsilosis ATCC 141095 by broth macro dilution method | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20 | Synthesis and antifungal activity of new azole derivatives containing an N-acylmorpholine ring. |
| AID362236 | Inhibition of hepatic CYP1A2 expressed in insect microsomes at 1 uM | 2008 | Bioorganic & medicinal chemistry, Aug-15, Volume: 16, Issue:16 | Synthesis, biological evaluation, and molecular modeling studies of methylene imidazole substituted biaryls as inhibitors of human 17alpha-hydroxylase-17,20-lyase (CYP17)--part II: Core rigidification and influence of substituents at the methylene bridge. |
| AID376051 | Antifungal activity against Cryptococcus neoformans ATCC 32264 by agar dilution method | 1999 | Journal of natural products, Oct, Volume: 62, Issue:10 | In vitro evaluation of antifungal properties of phenylpropanoids and related compounds acting against dermatophytes. |
| AID669126 | Antimicrobial activity against Malassezia pachydermatis infected in CD-1 mouse model of dandruff assessed as improvement in skin appearance at 2% cream administered once daily for 6 days measured daily for 20 days | 2012 | Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7 | Molecular cloning, characterization, and inhibition studies of a β-carbonic anhydrase from Malassezia globosa, a potential antidandruff target. |
| AID1450068 | Inhibition of recombinant human CYP3A4 expressed in insect cells using DBOMF as substrate pretreated for 10 mins followed by substrate addition measured every minute for 15 mins in presence of NADP+ by fluorescence assay | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11 | Cytochrome P450 binding studies of novel tacrine derivatives: Predicting the risk of hepatotoxicity. |
| AID1474081 | AUC in human at 200 mg, po QD after 24 hrs | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1 | A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
| AID244398 | In vitro IC50 ratio against human CYP11B1 to that of human CYP11B2 | 2005 | Journal of medicinal chemistry, Mar-10, Volume: 48, Issue:5 | Synthesis and evaluation of (pyridylmethylene)tetrahydronaphthalenes/-indanes and structurally modified derivatives: potent and selective inhibitors of aldosterone synthase. |
| AID1156682 | Antifungal activity against Candida albicans MTCC 227 assessed as zone of inhibition at 1 mg/disc after 48 hrs incubation by disc diffusion assay | 2014 | European journal of medicinal chemistry, Aug-18, Volume: 83 | Synthesis of new class of spirocarbocycle derivatives by multicomponent domino reaction and their evaluation for antimicrobial, anticancer activity and molecular docking studies. |
| AID49637 | Minimum inhibitory concentration of compound for antifungal activity against Candida albicans 4 | 2000 | Bioorganic & medicinal chemistry letters, Oct-02, Volume: 10, Issue:19 | Novel antifungals based on 4-substituted imidazole: a combinatorial chemistry approach to lead discovery and optimization. |
| AID633911 | Antifungal activity against Candida albicans PYCC 3436 at 10 ug/mL after 72 hrs by agar cup plate method | 2012 | European journal of medicinal chemistry, Jan, Volume: 47, Issue:1 | Isoxazoles incorporated N-substituted decahydroquinolines: a precursor to the next generation antimicrobial drug. |
| AID1467468 | Antifungal activity against Fusarium moniliforme at 75 ug/ml after 48 hrs by agar well diffusion method | 2017 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 27, Issue:14 | Synthesis, SAR and molecular docking studies of benzo[d]thiazole-hydrazones as potential antibacterial and antifungal agents. |
| AID42858 | Inhibition of Candida albicans ATCC 90028 for 48 hours in vitro. | 2001 | Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17 | 3-Phenyl-5-acyloxymethyl-2H,5H-furan-2-ones: synthesis and biological activity of a novel group of potential antifungal drugs. |
| AID395653 | Antifungal activity against Cryptococcus neoformans ATCC 32264 assessed as growth inhibition at 50 uM after 48 hrs | 2009 | European journal of medicinal chemistry, Jan, Volume: 44, Issue:1 | Penetratin and derivatives acting as antifungal agents. |
| AID1103201 | Antifungal activity against Fusarium equiseti (CE181) after 48 to 72 hr | 2004 | Journal of agricultural and food chemistry, Jun-02, Volume: 52, Issue:11 | Antifungal chalcones and new caffeic acid esters from Zuccagnia punctata acting against soybean infecting fungi. |
| AID1238920 | Antifungal activity against Candida albicans WTBF-50 by microbroth dilution method | 2015 | Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17 | Synthesis and antifungal evaluation of head-to-head and head-to-tail bisamidine compounds. |
| AID242626 | In vitro inhibition of [14C]deoxycorticosterone binding to human cytochrome P450 11B2 expressed in hamster V79 MZh cells | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Synthesis and evaluation of imidazolylmethylenetetrahydronaphthalenes and imidazolylmethyleneindanes: potent inhibitors of aldosterone synthase. |
| AID1263198 | Displacement of [3H}-MIB from rat prostate cytosol androgen receptor assessed as relative binding affinity | 2015 | Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24 | Synthesis and activity of novel 16-dehydropregnenolone acetate derivatives as inhibitors of type 1 5α-reductase and on cancer cell line SK-LU-1. |
| AID391508 | Antifungal activity against Neurospora crassa ATCC 9279 after 48 hrs by spectrophotometry | 2008 | Journal of natural products, Oct, Volume: 71, Issue:10 | Evidence for the mechanism of action of the antifungal phytolaccoside B isolated from Phytolacca tetramera Hauman. |
| AID632560 | Antibacterial activity against Bacillus subtilis at 200 ug/mL after 24 hrs by agar cup diffusion method | 2011 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 21, Issue:24 | A new antifungal briarane diterpenoid from the gorgonian Junceella juncea Pallas. |
| AID262557 | Antifungal activity against Trichophyton mentagrophytes | 2006 | Journal of medicinal chemistry, Apr-20, Volume: 49, Issue:8 | Structure-based optimization of azole antifungal agents by CoMFA, CoMSIA, and molecular docking. |
| AID53248 | Ability to inhibit the C17,20-lyase enzyme by 50% using 17-alpha-hydroxyprogesterone as substrate. | 1995 | Journal of medicinal chemistry, Jun-23, Volume: 38, Issue:13 | Novel steroidal inhibitors of human cytochrome P45017 alpha (17 alpha-hydroxylase-C17,20-lyase): potential agents for the treatment of prostatic cancer. |
| AID1103207 | Antifungal activity against Macrophomina phaseolina isolate CE173 after 48 to 72 hr | 2004 | Journal of agricultural and food chemistry, Jun-02, Volume: 52, Issue:11 | Antifungal chalcones and new caffeic acid esters from Zuccagnia punctata acting against soybean infecting fungi. |
| AID664302 | Antifungal activity against Aspergillus clavatus MTCC 1323 at 100 ug/disc by paper disc diffusion technique | 2012 | European journal of medicinal chemistry, Jul, Volume: 53 | Synthesis of benzimidazolyl-1,3,4-oxadiazol-2ylthio-N-phenyl (benzothiazolyl) acetamides as antibacterial, antifungal and antituberculosis agents. |
| AID456070 | Antifungal activity against Aspergillus flavus ATCC 9643 after 72 hrs by serial dilution method | 2010 | Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1 | Novel 4-thiazolidinone derivatives as potential antifungal and antibacterial drugs. |
| AID1176163 | Inhibition of human recombinant MDR1 in cell membrane fraction preincubated for 5 mins measured after 40 mins by Pgp-Glo luciferase assay | 2015 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2 | Investigating the binding interactions of the anti-Alzheimer's drug donepezil with CYP3A4 and P-glycoprotein. |
| AID530732 | Antifungal activity against Candida albicans ATCC 14053 at 9.4 uM after 48 hrs by CLSI method | 2008 | Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7 | Potent in vitro antifungal activities of naturally occurring acetylenic acids. |
| AID405049 | Antifungal activity against Sporothrix schenckii P26187 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by Sensititre YeastOne method | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods. |
| AID419365 | Antifungal activity against Aspergillus niger after 48 hrs by microdilution susceptibility method | 2009 | European journal of medicinal chemistry, May, Volume: 44, Issue:5 | Synthesis and bioassay of a new class of heterocycles pyrrolyl oxadiazoles/thiadiazoles/triazoles. |
| AID420662 | Antifungal activity against Candida parapsilosis by micro-broth dilution method | 2009 | European journal of medicinal chemistry, May, Volume: 44, Issue:5 | Design, synthesis, and biological evaluation of novel triazole derivatives as inhibitors of cytochrome P450 14alpha-demethylase. |
| AID49269 | In vitro antifungal activity against 40 strains at pH 7.2 minimum inhibitory concentration | 2002 | Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13 | Antifungal agents. 10. New derivatives of 1-[(aryl)[4-aryl-1H-pyrrol-3-yl]methyl]-1H-imidazole, synthesis, anti-candida activity, and quantitative structure-analysis relationship studies. |
| AID519281 | Antifungal activity against Candida krusei ATCC 6258 by AFST-EUCAST method | 2008 | Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3 | Reliability of the WIDERYST susceptibility testing system for detection of in vitro antifungal resistance in yeasts. |
| AID161281 | Inhibition of human Potassium channel HERG expressed in mammalian cells | 2003 | Bioorganic & medicinal chemistry letters, Aug-18, Volume: 13, Issue:16 | Prediction of hERG potassium channel affinity by traditional and hologram qSAR methods. |
| AID644182 | Antifungal activity against Trichoderma viride IAM 5061 after 72 hrs by serial dilution method | 2012 | Bioorganic & medicinal chemistry, Feb-15, Volume: 20, Issue:4 | Synthesis of novel sulfonamide-1,2,4-triazoles, 1,3,4-thiadiazoles and 1,3,4-oxadiazoles, as potential antibacterial and antifungal agents. Biological evaluation and conformational analysis studies. |
| AID362235 | Inhibition of hepatic CYP3A4 expressed in insect microsomes at 1 uM | 2008 | Bioorganic & medicinal chemistry, Aug-15, Volume: 16, Issue:16 | Synthesis, biological evaluation, and molecular modeling studies of methylene imidazole substituted biaryls as inhibitors of human 17alpha-hydroxylase-17,20-lyase (CYP17)--part II: Core rigidification and influence of substituents at the methylene bridge. |
| AID1079945 | Animal toxicity known. [column 'TOXIC' in source] | |||
| AID449696 | Antifungal activity against Aspergillus niger NCIM 596 after 48 hrs by microdilution susceptibility method | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11 | Synthesis, antimicrobial and antioxidant activities of substituted pyrazoles, isoxazoles, pyrimidine and thioxopyrimidine derivatives. |
| AID588208 | Literature-mined public compounds from Lowe et al phospholipidosis modelling dataset | 2010 | Molecular pharmaceutics, Oct-04, Volume: 7, Issue:5 | Predicting phospholipidosis using machine learning. |
| AID405100 | Antimicrobial activity against Absidia corymbifera after 24 hrs | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | In vitro susceptibilities of 217 clinical isolates of zygomycetes to conventional and new antifungal agents. |
| AID652429 | Inhibition of human CYP11B2 expressed in hamster V79 MZ cells using [3H] 11 deoxycorticosterone as substrate by HPLC radioflow detector | 2011 | ACS medicinal chemistry letters, Aug-11, Volume: 2, Issue:8 | Optimization of the First Selective Steroid-11β-hydroxylase (CYP11B1) Inhibitors for the Treatment of Cortisol Dependent Diseases. |
| AID566949 | Antifungal activity against Candida albicans ATCC 10231 assessed as inhibition of fungal growth at 50 uM after 24 hrs by microplate analysis | 2011 | European journal of medicinal chemistry, Jan, Volume: 46, Issue:1 | Penetratin analogues acting as antifungal agents. |
| AID249258 | Antifungal activity to cause 99% reduction of surviving cells in 90% isolates | 2004 | Journal of medicinal chemistry, Jul-29, Volume: 47, Issue:16 | Imidazole analogues of fluoxetine, a novel class of anti-Candida agents. |
| AID477747 | Antimicrobial activity against Candida parapsilosis ATCC 22019 after 24 hrs | 2010 | European journal of medicinal chemistry, Apr, Volume: 45, Issue:4 | An eco-friendly synthesis and antimicrobial activities of dihydro-2H-benzo- and naphtho-1,3-oxazine derivatives. |
| AID1171980 | Antibacterial activity against Enterobacter aerogenes MTCC 111 assessed as zone of inhibition at 1 mg/disc after 24 hrs by disc diffusion method | 2015 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2 | Facile and diastereoselective synthesis of 3,2'-spiropyrrolidine-oxindoles derivatives, their molecular docking and antiproliferative activities. |
| AID290149 | Antifungal activity against Candida albicans after 48 hrs by MTT colorimetric method | 2007 | European journal of medicinal chemistry, Apr, Volume: 42, Issue:4 | Synthesis and antimicrobial activities of Schiff bases derived from 5-chloro-salicylaldehyde. |
| AID262546 | Antifungal activity against Candida albicans | 2006 | Journal of medicinal chemistry, Apr-20, Volume: 49, Issue:8 | Structure-based optimization of azole antifungal agents by CoMFA, CoMSIA, and molecular docking. |
| AID48614 | Evaluation of In vitro antifungal activity against Candida tropicalis 2.11 by broth macro dilution method | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20 | Synthesis and antifungal activity of new azole derivatives containing an N-acylmorpholine ring. |
| AID678716 | Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using diethoxyfluorescein as substrate after 30 mins | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
| AID463749 | Inhibition of human recombinant aromatase at 3 uM | 2010 | Journal of natural products, Feb-26, Volume: 73, Issue:2 | The taiwaniaquinoids: a review. |
| AID674800 | Antifungal activity against Candida albicans after 48 hrs by microtiter broth dilution method | 2012 | European journal of medicinal chemistry, Sep, Volume: 55 | Laurene-type sesquiterpenes from the Red Sea red alga Laurencia obtusa as potential antitumor-antimicrobial agents. |
| AID1557085 | Antifungal activity against Candida albicans ATCC 90028 assessed as reduction in fungal cell growth incubated for 48 hrs by MTT based broth double dilution method | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Antifungal activity, mode of action variability, and subcellular distribution of coumarin-based antifungal azoles. |
| AID582796 | Antifungal activity against Candida albicans isolate 6 by broth microdilution method | 2010 | Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11 | Identification and characterization of four azole-resistant erg3 mutants of Candida albicans. |
| AID334234 | Antimicrobial activity against Trichophyton mentagrophytes NCPF 224 after 10 days by microdilution technique | 2002 | Journal of natural products, Apr, Volume: 65, Issue:4 | Antimicrobial activities of a new schizozygane indoline alkaloid from Schizozygia coffaeoides and the revised structure of isoschizogaline. |
| AID125964 | Minimum inhibitory concentration against Microsporum nanum | 2004 | Bioorganic & medicinal chemistry letters, Feb-09, Volume: 14, Issue:3 | Synthesis and antifungal activities of phenylenedithioureas. |
| AID243919 | In vitro inhibition against bovine cytochrome P450 11B with 200 uM corticosterone | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Synthesis and evaluation of imidazolylmethylenetetrahydronaphthalenes and imidazolylmethyleneindanes: potent inhibitors of aldosterone synthase. |
| AID519282 | Antifungal activity against Candida krusei ATCC 6258 by CLSI M27-A2 microdilution method | 2008 | Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3 | Reliability of the WIDERYST susceptibility testing system for detection of in vitro antifungal resistance in yeasts. |
| AID514963 | Inhibition of CYP24A1 in rat kidney mitochondria | 2010 | European journal of medicinal chemistry, Oct, Volume: 45, Issue:10 | Synthesis and CYP24A1 inhibitory activity of (E)-2-(2-substituted benzylidene)- and 2-(2-substituted benzyl)-6-methoxy-tetralones. |
| AID452386 | Antimicrobial activity against Yarrowia lipolytica after 48 hrs | 2009 | Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23 | Side chain azasteroids and thiasteroids as sterol methyltransferase inhibitors in ergosterol biosynthesis. |
| AID280107 | Inhibition of human recombinant aromatase | 2007 | Journal of natural products, Mar, Volume: 70, Issue:3 | Potential cancer chemopreventive in vitro activities of monomeric xanthone derivatives from the marine algicolous fungus Monodictys putredinis. |
| AID375407 | Antifungal activity against Candida albicans ATCC 10231 at 100 ug/mL after 24 hrs by disk diffusion method | 2009 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13 | Regioselective synthesis and biological evaluation of bis(indolyl)methane derivatized 1,4-disubstituted 1,2,3-bistriazoles as anti-infective agents. |
| AID454781 | Antifungal activity against Trichophyton rubrum C113 after 48 hrs by broth microdilution technique | 2009 | Bioorganic & medicinal chemistry, Nov-01, Volume: 17, Issue:21 | 5-Nitrofuranes and 5-nitrothiophenes with anti-Trypanosoma cruzi activity and ability to accumulate squalene. |
| AID405098 | Antimicrobial activity against Mucor circinelloides after 24 hrs | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | In vitro susceptibilities of 217 clinical isolates of zygomycetes to conventional and new antifungal agents. |
| AID551091 | Antifungal activity against Aspergillus flavus at 1000 ug/mL after 72 hrs by agar diffusion assay | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1 | 3-[Benzimidazo- and 3-[benzothiadiazoleimidazo-(1,2-c)quinazolin-5-yl]-2H-chromene-2-ones as potent antimicrobial agents. |
| AID687501 | Antifungal activity against Candida tropicalis after 48 hrs by NCCLS broth microdilution method | 2012 | Bioorganic & medicinal chemistry, Oct-15, Volume: 20, Issue:20 | Structure-activity relationship study of nitrosopyrimidines acting as antifungal agents. |
| AID138455 | In vivo inhibitory activity against arachidonic acid(AA) ear edema at a dose of 100 ug/ear | 1992 | Journal of medicinal chemistry, Aug-21, Volume: 35, Issue:17 | Novel 1-(pyridylphenyl)-1-phenyl-2-imidazolylethanols with topical antiinflammatory activity. |
| AID765640 | Fungistatic activity against Candida albicans NRRLY 477 after 24 hrs by two-fold serial dilution assay | 2013 | European journal of medicinal chemistry, Sep, Volume: 67 | Synthesis of thiosemicarbazones derived from N-(4-hippuric acid)thiosemicarbazide and different carbonyl compounds as antimicrobial agents. |
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| AID1467472 | Antifungal activity against Fusarium oxysporum at 75 ug/ml after 48 hrs by agar well diffusion method | 2017 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 27, Issue:14 | Synthesis, SAR and molecular docking studies of benzo[d]thiazole-hydrazones as potential antibacterial and antifungal agents. |
| AID1129508 | Antimicrobial activity against Aspergillus niger at 50 ug/well after 48 hrs by agar well diffusion method | 2014 | European journal of medicinal chemistry, Apr-22, Volume: 77 | Synthesis, antimicrobial and cytotoxic activities of pyrimidinyl benzoxazole, benzothiazole and benzimidazole. |
| AID311859 | Inhibition of human CYP3A4 expressed in Escherichia coli assessed as inhibition of nifedipine oxidation | 2007 | Journal of natural products, Dec, Volume: 70, Issue:12 | Cytochrome P3A4 inhibitors and other constituents of Fibraurea tinctoria. |
| AID555823 | Ratio of MIC50 for Candida albicans 5674 to MIC50 for cdr1/cdr1/cdr2/cdr2 deficient Candida albicans STY31 | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | Relative contributions of the Candida albicans ABC transporters Cdr1p and Cdr2p to clinical azole resistance. |
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| AID1130390 | Antifungal activity against Candida albicans assessed as growth inhibition in sabouraud broth after 14 days in presence of 10% inactivated bovine serum | 1979 | Journal of medicinal chemistry, Aug, Volume: 22, Issue:8 | Antimycotic imidazoles. part 4. Synthesis and antifungal activity of ketoconazole, a new potent orally active broad-spectrum antifungal agent. |
| AID503308 | Antiproliferative activity against human PC3 cells at 30 uM after 120 hrs by MTT assay relative to DMSO | 2006 | Nature chemical biology, Jun, Volume: 2, Issue:6 | Identifying off-target effects and hidden phenotypes of drugs in human cells. |
| AID586924 | Antileishmanial activity against tafenoquine-resistant promastigotes of Leishmania major R4 assessed as inhibition of parasite growth after 72 hrs by MTT assay | 2011 | Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3 | Increased glycolytic ATP synthesis is associated with tafenoquine resistance in Leishmania major. |
| AID633961 | Antifungal activity against Aspergillus flavus ATCC 9643 incubated for 72 hrs followed by serial sub-cultivation for 72 hrs by serial dilution technique | 2011 | Bioorganic & medicinal chemistry, Dec-15, Volume: 19, Issue:24 | Novel (E)-1-(4-methyl-2-(alkylamino)thiazol-5-yl)-3-arylprop-2-en-1-ones as potent antimicrobial agents. |
| AID1223621 | Inhibition of CYP3A4 activity in human liver microsomes assessed as dibenzo fluuorescene oxidation up to 40 uM | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4 | Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID594164 | Antimicrobial activity against Candida albicans NRRL Y-477 after 48 hrs by agar well diffusion method | 2011 | European journal of medicinal chemistry, May, Volume: 46, Issue:5 | Synthesis, antimicrobial, antioxidant, anti-hemolytic and cytotoxic evaluation of new imidazole-based heterocycles. |
| AID407003 | Antimicrobial activity against Candida albicans FH1 at planktonic cell density of 10'3 cells/ml after 48 hrs by XTT assay | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | Role for cell density in antifungal drug resistance in Candida albicans biofilms. |
| AID494001 | Antifungal activity against Candida albicans ATCC 10231 assessed as inhibition of fungal growth at 12.5 uM | 2010 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 20, Issue:16 | New antifungal peptides. Synthesis, bioassays and initial structure prediction by CD spectroscopy. |
| AID406864 | Antimicrobial activity against Candida albicans GDH2346 dissociated biofilms at cell density of 10'3 cells/ml after 48 hrs by XTT assay | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | Role for cell density in antifungal drug resistance in Candida albicans biofilms. |
| AID600770 | Antifungal activity against Penicillium ochrochloron ATCC 9112 after 72 hrs by serial dilution method | 2011 | Bioorganic & medicinal chemistry, May-15, Volume: 19, Issue:10 | Thiazole-based chalcones as potent antimicrobial agents. Synthesis and biological evaluation. |
| AID290144 | Antibacterial activity against Bacillus subtilis after 24 hrs by MTT colorimetric method | 2007 | European journal of medicinal chemistry, Apr, Volume: 42, Issue:4 | Synthesis and antimicrobial activities of Schiff bases derived from 5-chloro-salicylaldehyde. |
| AID572695 | Binding affinity to Mycobacterium smegmatis ATCC 700084 CYP164A2 at pH7.5 | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | Identification, characterization, and azole-binding properties of Mycobacterium smegmatis CYP164A2, a homolog of ML2088, the sole cytochrome P450 gene of Mycobacterium leprae. |
| AID208352 | Maximum enhancement of styrene oxide hydrolase activity was reported at compound concentration of 1e-3 M | 1985 | Journal of medicinal chemistry, Aug, Volume: 28, Issue:8 | Structural features of imidazole derivatives that enhance styrene oxide hydrolase activity in rat hepatic microsomes. |
| AID1557084 | Antifungal activity against Candida dubliniensis T-99 assessed as reduction in fungal cell growth incubated for 24 hrs by MTT based broth double dilution method | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Antifungal activity, mode of action variability, and subcellular distribution of coumarin-based antifungal azoles. |
| AID463750 | Inhibition of human recombinant aromatase at 0.3 uM | 2010 | Journal of natural products, Feb-26, Volume: 73, Issue:2 | The taiwaniaquinoids: a review. |
| AID155490 | In vitro antifungal activity against Phialophora verrucosa | 1984 | Journal of medicinal chemistry, Jul, Volume: 27, Issue:7 | Antimycotic azoles. 7. Synthesis and antifungal properties of a series of novel triazol-3-ones. |
| AID303381 | Cytotoxicity against human THP1 cells after 48 hrs | 2007 | Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24 | In vivo anti-Chagas vinylthio-, vinylsulfinyl-, and vinylsulfonylbenzofuroxan derivatives. |
| AID502080 | Inhibition of 17,20-lyase activity of rat testicular microsomal P450-17alpha | 2010 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 20, Issue:17 | Synthesis and biochemical evaluation of a range of (4-substituted phenyl)sulfonate derivatives of 4-hydroxybenzyl imidazole-based compounds as potent inhibitors of 17alpha-hydroxylase/17,20-lyase (P45017alpha) derived from rat testicular microsomes. |
| AID348154 | Cytotoxicity against mouse J774 cells at 400 uM after 48 hrs by MTT assay | 2009 | Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2 | Synthesis, trypanocidal activity and docking studies of novel quinoxaline-N-acylhydrazones, designed as cruzain inhibitors candidates. |
| AID50300 | Tested for minimum inhibitory concentration against Candida krusei 132 (C.k) at pH 6.5. | 1994 | Journal of medicinal chemistry, Jun-24, Volume: 37, Issue:13 | Derivatives of a novel cyclopeptolide. 1. Synthesis, antifungal activity, and structure-activity relationships. |
| AID640967 | Antifungal activity against Aspergillus niger NCIM 548 after 48 hrs by agar well diffusion assay | 2012 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2 | Synthesis, characterization and in vitro biological evaluation of some novel diarylsulfonylureas as potential cytotoxic and antimicrobial agents. |
| AID452382 | Inhibition of Yarrowia lipolytica 24-SMT assessed as 14-alpha-methylergosta-8,24(28)-dien-3beta,6alpha-di-trimethylsilyl derivative at 0.2 ug/mL after 48 hrs by GC-MS analysis relative to untreated control | 2009 | Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23 | Side chain azasteroids and thiasteroids as sterol methyltransferase inhibitors in ergosterol biosynthesis. |
| AID1209974 | Inhibition of CYP3A4 in human liver microsomes using midazolam as substrate after 8 mins by LC-MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5 | Identifying a selective substrate and inhibitor pair for the evaluation of CYP2J2 activity. |
| AID179677 | Tested for efficacy of compound in experimental vaginal candidosis (rat) after oral treatment at dosage of 2x 150 mg kg e-1 | 1994 | Journal of medicinal chemistry, Jun-24, Volume: 37, Issue:13 | Derivatives of a novel cyclopeptolide. 1. Synthesis, antifungal activity, and structure-activity relationships. |
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| AID420078 | Antifungal activity against Cryptococcus neoformans CAP67 after 24 hrs by broth microdilution assay | 2009 | Bioorganic & medicinal chemistry, Jun-01, Volume: 17, Issue:11 | Bulky 1,4-benzoxazine derivatives with antifungal activity. |
| AID370299 | Effect on CYP3A4 in human liver assessed as nifedipine oxidation at 100 uM relative to control | 2006 | PLoS medicine, Nov, Volume: 3, Issue:11 | OPC-67683, a nitro-dihydro-imidazooxazole derivative with promising action against tuberculosis in vitro and in mice. |
| AID1103202 | Antifungal activity against Diaporthe longicolla CE117 after 48 to 72 hr | 2004 | Journal of agricultural and food chemistry, Jun-02, Volume: 52, Issue:11 | Antifungal chalcones and new caffeic acid esters from Zuccagnia punctata acting against soybean infecting fungi. |
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| AID670548 | Inhibition of CYP3A4 at 10 uM | 2012 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14 | Synthesis and evaluation of novel potent HCV NS5A inhibitors. |
| AID717027 | Antifungal activity against Candida parapsilosis NRRL Y-12696 after 24 hrs by microdilution susceptibility assay | 2012 | European journal of medicinal chemistry, Dec, Volume: 58 | Synthesis and biological evaluation of some hydrazone derivatives as new anticandidal and anticancer agents. |
| AID532550 | Antifungal activity against Saccharomyces cerevisiae BY4741 harboring human CYP51 by broth microdilution method | 2008 | Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10 | Differential azole antifungal efficacies contrasted using a Saccharomyces cerevisiae strain humanized for sterol 14 alpha-demethylase at the homologous locus. |
| AID572704 | Binding affinity to human CYP51 | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | Identification, characterization, and azole-binding properties of Mycobacterium smegmatis CYP164A2, a homolog of ML2088, the sole cytochrome P450 gene of Mycobacterium leprae. |
| AID1179289 | Antimicrobial activity against Malassezia pachydermatis after 48 to 72 hrs by two fold dilution method | 2014 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 24, Issue:14 | Synthesis, antimicrobial and molecular docking studies of enantiomerically pure N-alkylated β-amino alcohols from phenylpropanolamines. |
| AID363723 | Antimicrobial activity against Candida albicans ATCC 10231 at 6.25 ug/ml after 24 hrs | 2008 | Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17 | In vitro antifungal activity of polyfunctionalized 2-(hetero)arylquinolines prepared through imino Diels-Alder reactions. |
| AID624628 | Drug-stimulated Pgp ATPase activity ratio determined in MDR1-Sf9 cell membranes with test compound at a concentration of 20uM | 2001 | The Journal of pharmacology and experimental therapeutics, Nov, Volume: 299, Issue:2 | Rational use of in vitro P-glycoprotein assays in drug discovery. |
| AID307404 | Cytotoxicity against human HepG2 cells by neutral red uptake assay | 2007 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12 | Discovery of novel indazole-linked triazoles as antifungal agents. |
| AID602592 | Antifungal activity against Candida albicans after 12 hrs by agar dilution method | 2011 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 21, Issue:13 | Antifungal quinazolinones from marine-derived Bacillus cereus and their preparation. |
| AID420664 | Antifungal activity against Trichophyton rubrum by micro-broth dilution method | 2009 | European journal of medicinal chemistry, May, Volume: 44, Issue:5 | Design, synthesis, and biological evaluation of novel triazole derivatives as inhibitors of cytochrome P450 14alpha-demethylase. |
| AID214262 | In vitro antifungal activity against Trichophyton mentagrophytes ATCC 9533 | 1988 | Journal of medicinal chemistry, Oct, Volume: 31, Issue:10 | Studies on antifungal agents. 23. Novel substituted 3,5-diphenyl-3-(1H-imidazol-1-ylmethyl)- 2-alkylisoxazolidine derivatives. |
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| AID644183 | Antifungal activity against Aspergillus fumigatus human isolate after 72 hrs by serial dilution method | 2012 | Bioorganic & medicinal chemistry, Feb-15, Volume: 20, Issue:4 | Synthesis of novel sulfonamide-1,2,4-triazoles, 1,3,4-thiadiazoles and 1,3,4-oxadiazoles, as potential antibacterial and antifungal agents. Biological evaluation and conformational analysis studies. |
| AID47866 | Evaluation of In vitro antifungal activity against Candida parapsilosis ATCC 22019 by broth macro dilution method | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20 | Synthesis and antifungal activity of new azole derivatives containing an N-acylmorpholine ring. |
| AID590623 | Antifungal activity against Curvularia lunata assessed as zone of inhibition at 200 ug/ml after 48 hrs by disc diffusion method | 2011 | European journal of medicinal chemistry, Apr, Volume: 46, Issue:4 | Synthesis and biological activity of 2-(bis((1,3,4-oxadiazolyl/1,3,4-thiadiazolyl)methylthio)methylene)malononitriles. |
| AID395377 | Antifungal activity against Kluyveromyces fragilis NRRL 2415 at 1 ug after 72 hrs by disk diffusion method | 2009 | European journal of medicinal chemistry, Jan, Volume: 44, Issue:1 | Synthesis, Raman, FT-IR, NMR spectroscopic data and antimicrobial activity of mixed aza-oxo-thia macrocyclic compounds. |
| AID48639 | Evaluation of In vitro antifungal activity against Candida tropicalis 50 by broth macro dilution method | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20 | Synthesis and antifungal activity of new azole derivatives containing an N-acylmorpholine ring. |
| AID48611 | In vitro antifungal activity against Candida tropicalis | 1984 | Journal of medicinal chemistry, Jul, Volume: 27, Issue:7 | Antimycotic azoles. 7. Synthesis and antifungal properties of a series of novel triazol-3-ones. |
| AID554717 | Antimicrobial activity against Saccharomyces cerevisiae isolate ADdelta overexpressing Abc1p after 48 hrs by liquid microdilution assay | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2 | Abc1p is a multidrug efflux transporter that tips the balance in favor of innate azole resistance in Candida krusei. |
| AID555818 | Antifungal activity against cdr1/cdr1 deficient Candida albicans STY19 after 48 hrs | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | Relative contributions of the Candida albicans ABC transporters Cdr1p and Cdr2p to clinical azole resistance. |
| AID618044 | Antifungal activity against 10'5 CFU/mL Aspergillus clavatus MTCC 1323 at 100 ug/ml after 48 hrs by disc diffusion technique | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Synthesis and studies of novel 2-(4-cyano-3-trifluoromethylphenyl amino)-4-(quinoline-4-yloxy)-6-(piperazinyl/piperidinyl)-s-triazines as potential antimicrobial, antimycobacterial and anticancer agents. |
| AID519283 | Antifungal activity against Candida krusei ATCC 6258 by WIDERYST method | 2008 | Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3 | Reliability of the WIDERYST susceptibility testing system for detection of in vitro antifungal resistance in yeasts. |
| AID32670 | In vitro inhibition of Absidia corymbifera 272 growth for 48 hours. | 2001 | Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17 | 3-Phenyl-5-acyloxymethyl-2H,5H-furan-2-ones: synthesis and biological activity of a novel group of potential antifungal drugs. |
| AID341134 | Antifungal activity against Saccharomycopsis guttulata isolates from feeding stuff by NCCLS M27-A2 method | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8 | Cross-resistance to medical and agricultural azole drugs in yeasts from the oropharynx of human immunodeficiency virus patients and from environmental Bavarian vine grapes. |
| AID1232935 | Inhibition of CYP19 (unknown origin) using O-benzyl fluorescein benzyl ester substrate preincubated for 10 mins by fluorimetric analysis relative to control | 2015 | Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13 | Synthesis and molecular docking of 1,2,3-triazole-based sulfonamides as aromatase inhibitors. |
| AID456689 | Antifungal activity against Candida albicans ATCC 10231 assessed as inhibition of fungal growth at 100 uM after 24 hrs by microbroth dilution method | 2010 | Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1 | New small-size peptides possessing antifungal activity. |
| AID330519 | Toxicity against human HepG2 cells at 50 ug/ml | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Mar-13, Volume: 104, Issue:11 | High-throughput synergy screening identifies microbial metabolites as combination agents for the treatment of fungal infections. |
| AID463418 | Antimicrobial activity against Candida albicans after 24 hrs by liquid dilution method | 2010 | European journal of medicinal chemistry, Mar, Volume: 45, Issue:3 | Antimicrobial study of newly synthesized 6-substituted indolo[1,2-c]quinazolines. |
| AID1157294 | Antifungal activity against Cryptococcus neoformans 32609 assessed as growth inhibition by automatic microplate reader analysis | 2014 | Journal of natural products, May-23, Volume: 77, Issue:5 | Polyhydroxy cyclohexanols from a Dendrodochium sp. fungus associated with the sea cucumber Holothuria nobilis Selenka. |
| AID977599 | Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM | 2013 | Molecular pharmacology, Jun, Volume: 83, Issue:6 | Structure-based identification of OATP1B1/3 inhibitors. |
| AID287713 | Antitrypanosomatid activity against Trypanosoma cruzi Tulahuen 2 epimastigotes assessed as reduction of growth after 5 days | 2007 | Bioorganic & medicinal chemistry, Apr-01, Volume: 15, Issue:7 | Second generation of 5-ethenylbenzofuroxan derivatives as inhibitors of Trypanosoma cruzi growth: synthesis, biological evaluation, and structure-activity relationships. |
| AID1166504 | Inhibition of human prostate 5alpha-reductase type 2 assessed as conversion of [3H]testosterone to dihydrotestosterone | 2014 | Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21 | Effect of dehydroepiandrosterone derivatives on the activity of 5α-reductase isoenzymes and on cancer cell line PC-3. |
| AID449688 | Antifungal activity against Aspergillus niger NCIM 596 at 100 ug/disk after 48 hrs by agar disk diffusion method | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11 | Synthesis, antimicrobial and antioxidant activities of substituted pyrazoles, isoxazoles, pyrimidine and thioxopyrimidine derivatives. |
| AID564272 | Antifungal activity against Candida albicans isolate 108 harboring erg11 and erg5 double mutant after 48 hrs by broth microdilution method | 2010 | Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9 | A clinical isolate of Candida albicans with mutations in ERG11 (encoding sterol 14alpha-demethylase) and ERG5 (encoding C22 desaturase) is cross resistant to azoles and amphotericin B. |
| AID1328080 | Antifungal activity against Aspergillus niger assessed as inhibition of spore germination at 50 ug/well after 48 hrs by agar well diffusion method | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | Synthesis and antimicrobial activity of styryl/pyrrolyl/pyrazolyl sulfonylmethyl-1,3,4-oxadiazolyl amines and styryl/pyrrolyl/pyrazolyl sulfonylmethyl-1,3,4-thiadiazolyl amines. |
| AID315665 | Inhibition of recombinant CYP2D6 at 1 uM | 2008 | Bioorganic & medicinal chemistry, Feb-15, Volume: 16, Issue:4 | Synthesis, biological evaluation and molecular modelling studies of methyleneimidazole substituted biaryls as inhibitors of human 17alpha-hydroxylase-17,20-lyase (CYP17). Part I: Heterocyclic modifications of the core structure. |
| AID1171983 | Antibacterial activity against methicillin-resistant Staphylococcus aureus assessed as zone of inhibition at 1 mg/disc after 24 hrs by disc diffusion method | 2015 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2 | Facile and diastereoselective synthesis of 3,2'-spiropyrrolidine-oxindoles derivatives, their molecular docking and antiproliferative activities. |
| AID315658 | Inhibition of recombinant CYP1A2 at 10 uM | 2008 | Bioorganic & medicinal chemistry, Feb-15, Volume: 16, Issue:4 | Synthesis, biological evaluation and molecular modelling studies of methyleneimidazole substituted biaryls as inhibitors of human 17alpha-hydroxylase-17,20-lyase (CYP17). Part I: Heterocyclic modifications of the core structure. |
| AID611681 | Antibacterial activity against Escherichia coli at 0.05 mg by agar diffusion method | 2011 | Journal of natural products, Jul-22, Volume: 74, Issue:7 | Bioactive 11,20-epoxy-3,5(16)-diene briarane diterpenoids from the South China Sea gorgonian Dichotella gemmacea. |
| AID262554 | Antifungal activity against Microsporum gypseum | 2006 | Journal of medicinal chemistry, Apr-20, Volume: 49, Issue:8 | Structure-based optimization of azole antifungal agents by CoMFA, CoMSIA, and molecular docking. |
| AID606217 | Antifungal activity against Trichophyton rubrum after 7 days by micro-broth dilution method | 2011 | European journal of medicinal chemistry, Jul, Volume: 46, Issue:7 | Design, synthesis and antifungal activities of novel 1,2,4-triazole derivatives. |
| AID530578 | Antileishmanial activity against GFP-tagged at COOH terminus Leishmania infantum promastigotes overexpressing LiABCG6 assessed as cell viability after 72 hrs by MTT assay | 2008 | Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10 | Characterization of an ABCG-like transporter from the protozoan parasite Leishmania with a role in drug resistance and transbilayer lipid movement. |
| AID1155876 | Cytotoxicity against human PC3 cells assessed as growth inhibition at 50 uM after 48 hrs by SRB method | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Synthesis and cytotoxic effect on cancer cell lines and macrophages of novel progesterone derivatives having an ester or a carbamate function at C-3 and C-17. |
| AID415953 | Antimicrobial activity against Trichophyton rubrum by micro-broth dilution method | 2009 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6 | Design, synthesis, and biological evaluation of novel 1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluorophenyl)-3-substituted benzylamino-2-propanols. |
| AID768391 | Antifungal activity against Aspergillus clavatus MTCC 1323 by conventional broth microdilution method | 2013 | European journal of medicinal chemistry, Sep, Volume: 67 | Synthesis, antimicrobial and cytotoxic activities of some novel thiazole clubbed 1,3,4-oxadiazoles. |
| AID633950 | Antifungal activity against Aspergillus ochraceus ATCC 12066 after 72 hrs by serial dilution technique | 2011 | Bioorganic & medicinal chemistry, Dec-15, Volume: 19, Issue:24 | Novel (E)-1-(4-methyl-2-(alkylamino)thiazol-5-yl)-3-arylprop-2-en-1-ones as potent antimicrobial agents. |
| AID214424 | In vitro antifungal activity against Trichophyton rubrum ATCC 18762 | 1988 | Journal of medicinal chemistry, Oct, Volume: 31, Issue:10 | Studies on antifungal agents. 23. Novel substituted 3,5-diphenyl-3-(1H-imidazol-1-ylmethyl)- 2-alkylisoxazolidine derivatives. |
| AID687550 | Antifungal activity against Trichophyton rubrum CCC 110 by NCCLS broth microdilution method | 2012 | Bioorganic & medicinal chemistry, Oct-15, Volume: 20, Issue:20 | Structure-activity relationship study of nitrosopyrimidines acting as antifungal agents. |
| AID449589 | Inhibition of human CYP3A4 | 2009 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 19, Issue:18 | A novel class of highly potent multidrug resistance reversal agents: disubstituted adamantyl derivatives. |
| AID363715 | Antifungal activity against Aspergillus niger ATCC 9029 after 48 hrs by broth microdilution technique | 2008 | Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17 | In vitro antifungal activity of polyfunctionalized 2-(hetero)arylquinolines prepared through imino Diels-Alder reactions. |
| AID42877 | Inhibition of Candida krusei E28 growth for 48 hours in vitro. | 2001 | Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17 | 3-Phenyl-5-acyloxymethyl-2H,5H-furan-2-ones: synthesis and biological activity of a novel group of potential antifungal drugs. |
| AID50154 | Evaluation of In vitro antifungal activity against Candida krusei C64 by broth macro dilution method | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20 | Synthesis and antifungal activity of new azole derivatives containing an N-acylmorpholine ring. |
| AID566955 | Antifungal activity against Cryptococcus neoformans ATCC 32264 assessed as inhibition of fungal growth at 50 uM after 48 hrs by microplate analysis | 2011 | European journal of medicinal chemistry, Jan, Volume: 46, Issue:1 | Penetratin analogues acting as antifungal agents. |
| AID49432 | In vitro antifungal activity against 40 strains at pH 7.2, (percent of resistant species at 256 ug/mL) | 2002 | Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13 | Antifungal agents. 10. New derivatives of 1-[(aryl)[4-aryl-1H-pyrrol-3-yl]methyl]-1H-imidazole, synthesis, anti-candida activity, and quantitative structure-analysis relationship studies. |
| AID221160 | Inhibition of lanosterol 14-alpha-demethylase in hamster hepatic microsomes | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | Selective inhibition of mammalian lanosterol 14 alpha-demethylase: a possible strategy for cholesterol lowering. |
| AID1467464 | Antifungal activity against Aspergillus niger at 75 ug/ml after 48 hrs by agar well diffusion method | 2017 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 27, Issue:14 | Synthesis, SAR and molecular docking studies of benzo[d]thiazole-hydrazones as potential antibacterial and antifungal agents. |
| AID419357 | Antifungal activity against Aspergillus niger at 100 ug/disk after 48 hrs by agar disc-diffusion method | 2009 | European journal of medicinal chemistry, May, Volume: 44, Issue:5 | Synthesis and bioassay of a new class of heterocycles pyrrolyl oxadiazoles/thiadiazoles/triazoles. |
| AID540238 | Phospholipidosis-positive literature compound observed in mouse | |||
| AID750219 | Antifungal activity against Saccharomyces cerevisiae after 24 hrs by two fold serial dilution technique | 2013 | European journal of medicinal chemistry, Jun, Volume: 64 | Thiourea derivatives incorporating a hippuric acid moiety: synthesis and evaluation of antibacterial and antifungal activities. |
| AID582797 | Antifungal activity against Candida albicans isolate 14 by broth microdilution method | 2010 | Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11 | Identification and characterization of four azole-resistant erg3 mutants of Candida albicans. |
| AID211475 | The compound was tested for antifungal activity against Torulopsis glabrata MY1059 using agar dilution assay | 1987 | Journal of medicinal chemistry, Aug, Volume: 30, Issue:8 | Lysosomotropic agents. 7. Broad-spectrum antifungal activity of lysosomotropic detergents. |
| AID575117 | Antifungal activity against Madurella mycetomatis isolate 64 by XTT assay | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Madurella mycetomatis is not susceptible to the echinocandin class of antifungal agents. |
| AID532536 | Antifungal activity against Saccharomyces cerevisiae BY4741 harboring human CYP51 assessed as accumulation of ergosterol at 4 ug/ml (Rvb = 54+/- 0.82 %) | 2008 | Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10 | Differential azole antifungal efficacies contrasted using a Saccharomyces cerevisiae strain humanized for sterol 14 alpha-demethylase at the homologous locus. |
| AID50156 | In vitro evaluation of minimum inhibitory concentration against Candida krusei 70 | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20 | Synthesis and antifungal activity of new azole derivatives containing an N-acylmorpholine ring. |
| AID225406 | Percent decrease in plasma testosterone after 6 hr | 2000 | Journal of medicinal chemistry, Nov-02, Volume: 43, Issue:22 | Synthesis and evaluation of novel steroidal oxime inhibitors of P450 17 (17 alpha-hydroxylase/C17-20-lyase) and 5 alpha-reductase types 1 and 2. |
| AID43009 | Inhibition of Candida tropicalis 156 growth for 48 hours in vitro. | 2001 | Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17 | 3-Phenyl-5-acyloxymethyl-2H,5H-furan-2-ones: synthesis and biological activity of a novel group of potential antifungal drugs. |
| AID486236 | Antifungal activity against Saccharomyces cerevisiae ATCC 9763 after 48 hrs | 2010 | European journal of medicinal chemistry, Jun, Volume: 45, Issue:6 | Naftifine-analogues as anti-Trypanosoma cruzi agents. |
| AID1171994 | Antibacterial activity against methicillin-resistant Staphylococcus aureus assessed as inhibition of visual growth after 24 hrs | 2015 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2 | Facile and diastereoselective synthesis of 3,2'-spiropyrrolidine-oxindoles derivatives, their molecular docking and antiproliferative activities. |
| AID1075573 | Antimicrobial activity against Aspergillus ochraceus NRRL 3174 after 48 to 72 hrs by microbroth dilution method | 2014 | European journal of medicinal chemistry, Mar-03, Volume: 74 | Synthesis and biological evaluation of thiazoline derivatives as new antimicrobial and anticancer agents. |
| AID287717 | Ratio of IC50 for human THP1 cells to IC50 for Trypanosoma cruzi Tulahuen 2 epimastigotes | 2007 | Bioorganic & medicinal chemistry, Apr-01, Volume: 15, Issue:7 | Second generation of 5-ethenylbenzofuroxan derivatives as inhibitors of Trypanosoma cruzi growth: synthesis, biological evaluation, and structure-activity relationships. |
| AID362471 | Inhibition of human CYP17 expressed in Escherichia coli coexpressed with cytochrome P450 reductase | 2008 | Bioorganic & medicinal chemistry, Aug-15, Volume: 16, Issue:16 | Synthesis, biological evaluation, and molecular modeling studies of methylene imidazole substituted biaryls as inhibitors of human 17alpha-hydroxylase-17,20-lyase (CYP17)--part II: Core rigidification and influence of substituents at the methylene bridge. |
| AID242765 | In vitro inhibition of [14C]deoxycorticosterone binding to human cytochrome P450 11B1 expressed in hamster V79 MZh cells; nd= not determined | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Synthesis and evaluation of imidazolylmethylenetetrahydronaphthalenes and imidazolylmethyleneindanes: potent inhibitors of aldosterone synthase. |
| AID322154 | Antifungal activity against Candida albicans C 126-2000 after 48 hrs by CLSI M27-A2 method | 2008 | Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1 | N-Phenyl and N-phenylalkyl-maleimides acting against Candida spp.: time-to-kill, stability, interaction with maleamic acids. |
| AID407017 | Antimicrobial activity against Cdr1, Cdr2 and Mdr1 deficient Candida albicans DSY1050 intact biofilms after 48 hrs by XTT assay | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | Role for cell density in antifungal drug resistance in Candida albicans biofilms. |
| AID549051 | Antifungal activity against Candida albicans CA135 after 48 hrs by broth microdilution method | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | In vitro activities of retigeric acid B alone and in combination with azole antifungal agents against Candida albicans. |
| AID1110745 | Antifungal activity against Candida tropicalis 156 after 24 hr by microdilution broth method | 2002 | Farmaco (Societa chimica italiana : 1989), Feb, Volume: 57, Issue:2 | Ring substituted 3-phenyl-1-(2-pyrazinyl)-2-propen-1-ones as potential photosynthesis-inhibiting, antifungal and antimycobacterial agents. |
| AID48276 | Tested In vitro for antifungal activity against candida Spp (Candida glabrata, Candida krusei) at pH 7.2 | 2002 | Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13 | Antifungal agents. 10. New derivatives of 1-[(aryl)[4-aryl-1H-pyrrol-3-yl]methyl]-1H-imidazole, synthesis, anti-candida activity, and quantitative structure-analysis relationship studies. |
| AID53378 | Inhibition of rat testicular C17,20-Lyase | 1995 | Journal of medicinal chemistry, Oct-13, Volume: 38, Issue:21 | Esters of 3-pyridylacetic acid that combine potent inhibition of 17 alpha-hydroxylase/C17,20-lyase (cytochrome P45017 alpha) with resistance to esterase hydrolysis. |
| AID260492 | Functional activity at large conductance calcium-activated potassium channel in bovine smooth muscle cells | 2006 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 16, Issue:4 | Partial structures of ketoconazole as modulators of the large conductance calcium-activated potassium channel (BK(Ca)). |
| AID47890 | Evaluation of In vitro antifungal activity against Candida parapsilosis C74 by broth macro dilution method | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20 | Synthesis and antifungal activity of new azole derivatives containing an N-acylmorpholine ring. |
| AID70214 | Enhancement of epoxide hydrolase activity | 1985 | Journal of medicinal chemistry, Aug, Volume: 28, Issue:8 | Structural features of imidazole derivatives that enhance styrene oxide hydrolase activity in rat hepatic microsomes. |
| AID39401 | The compound was tested for antifungal activity against Aspergillus flavus MF0383 using agar dilution assay | 1987 | Journal of medicinal chemistry, Aug, Volume: 30, Issue:8 | Lysosomotropic agents. 7. Broad-spectrum antifungal activity of lysosomotropic detergents. |
| AID463419 | Antimicrobial activity against Trichoderma viride after 24 hrs by liquid dilution method | 2010 | European journal of medicinal chemistry, Mar, Volume: 45, Issue:3 | Antimicrobial study of newly synthesized 6-substituted indolo[1,2-c]quinazolines. |
| AID48256 | Inhibitory activity against Candida. species (40 clinical isolates), determined at pH-5.8 | 1995 | Journal of medicinal chemistry, Oct-13, Volume: 38, Issue:21 | Antifungal agents. 9. 3-Aryl-4-[alpha-(1H-imidazol-1-yl)arylmethyl]pyrroles: a new class of potent anti-Candida agents. |
| AID644191 | Antifungal activity against Aspergillus fumigatus human isolate treated for 72 hrs followed by sub-cultivated for 5 days by serial dilution method | 2012 | Bioorganic & medicinal chemistry, Feb-15, Volume: 20, Issue:4 | Synthesis of novel sulfonamide-1,2,4-triazoles, 1,3,4-thiadiazoles and 1,3,4-oxadiazoles, as potential antibacterial and antifungal agents. Biological evaluation and conformational analysis studies. |
| AID381188 | Antifungal activity against Cryptococcus neoformans 2 after 24 to 72 hrs by disk diffusion method | 1999 | Journal of natural products, Sep, Volume: 62, Issue:9 | Antimicrobial and antitumor activities of mycosporulone. |
| AID648035 | Antifungal activity against Saccharomyces cerevisiae by two fold serial dilution method | 2012 | European journal of medicinal chemistry, Apr, Volume: 50 | Regioselective synthesis and antimicrobial activities of some novel aryloxyacetic acid derivatives. |
| AID1281960 | Inhibition of recombinant human CYP3A4 at 10 uM by luminescence -based microplate reader assay | 2016 | European journal of medicinal chemistry, Apr-13, Volume: 112 | Rational design in search for 5-phenylhydantoin selective 5-HT7R antagonists. Molecular modeling, synthesis and biological evaluation. |
| AID619542 | Antifungal activity against Escherichia coli ATCC 10231 after 48 hrs by MTT assay | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10 | Tyrosyl-tRNA synthetase inhibitors as antibacterial agents: synthesis, molecular docking and structure-activity relationship analysis of 3-aryl-4-arylaminofuran-2(5H)-ones. |
| AID1557082 | Antifungal activity against Candida parapsilosis ATCC 22019 assessed as reduction in fungal cell growth incubated for 24 hrs by MTT based broth double dilution method | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Antifungal activity, mode of action variability, and subcellular distribution of coumarin-based antifungal azoles. |
| AID588210 | Human drug-induced liver injury (DILI) modelling dataset from Ekins et al | 2010 | Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 38, Issue:12 | A predictive ligand-based Bayesian model for human drug-induced liver injury. |
| AID511040 | Antimicrobial activity against Curvularia lunata NCIM 716 at 100 ug/disk after 48 hrs by agar disc-diffusion method | 2010 | European journal of medicinal chemistry, Sep, Volume: 45, Issue:9 | Synthesis and bioassay of aminosulfonyl-1,3,4-oxadiazoles and their interconversion to 1,3,4-thiadiazoles. |
| AID1328082 | Antifungal activity against Penicillium chrysogenum assessed as inhibition of spore germination at 12.5 ug/well after 48 hrs by agar well diffusion method | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | Synthesis and antimicrobial activity of styryl/pyrrolyl/pyrazolyl sulfonylmethyl-1,3,4-oxadiazolyl amines and styryl/pyrrolyl/pyrazolyl sulfonylmethyl-1,3,4-thiadiazolyl amines. |
| AID420212 | Antimicrobial activity against Staphylococcus aureus UFPEDA 01 after 20 hrs by twofold serial dilution technique | 2009 | European journal of medicinal chemistry, May, Volume: 44, Issue:5 | Synthesis, antimicrobial and cytotoxic activities of some 5-arylidene-4-thioxo-thiazolidine-2-ones. |
| AID405107 | Antimicrobial activity against Mucor sp. after assessed as percent of susceptible isolates after 24 hrs | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | In vitro susceptibilities of 217 clinical isolates of zygomycetes to conventional and new antifungal agents. |
| AID537736 | Antifungal activity against yeast AD1-8u expressing Candida albicans CaCdr1p by agar disk diffusion assay | 2010 | European journal of medicinal chemistry, Nov, Volume: 45, Issue:11 | Analysis of physico-chemical properties of substrates of ABC and MFS multidrug transporters of pathogenic Candida albicans. |
| AID405064 | Antifungal activity against Sporothrix schenckii P3287 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by Sensititre YeastOne method | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods. |
| AID220096 | The compound was evaluated for mean zone diameter (inhibition) against yeast at the concentration of 500 ug/mL | 1987 | Journal of medicinal chemistry, Aug, Volume: 30, Issue:8 | Lysosomotropic agents. 7. Broad-spectrum antifungal activity of lysosomotropic detergents. |
| AID254813 | Inhibitory concentration against human hepatic cytochrome P450 3A4 enzyme | 2005 | Journal of medicinal chemistry, Oct-20, Volume: 48, Issue:21 | Heteroaryl-substituted naphthalenes and structurally modified derivatives: selective inhibitors of CYP11B2 for the treatment of congestive heart failure and myocardial fibrosis. |
| AID1328079 | Antifungal activity against Aspergillus niger assessed as inhibition of spore germination at 25 ug/well after 48 hrs by agar well diffusion method | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | Synthesis and antimicrobial activity of styryl/pyrrolyl/pyrazolyl sulfonylmethyl-1,3,4-oxadiazolyl amines and styryl/pyrrolyl/pyrazolyl sulfonylmethyl-1,3,4-thiadiazolyl amines. |
| AID73612 | The compound was evaluated for mean zone diameter (inhibition) against yeast at the concentration of 1000 ug/mL | 1987 | Journal of medicinal chemistry, Aug, Volume: 30, Issue:8 | Lysosomotropic agents. 7. Broad-spectrum antifungal activity of lysosomotropic detergents. |
| AID49292 | Tested In vitro for antifungal activity at pH 5.8 | 2002 | Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13 | Antifungal agents. 10. New derivatives of 1-[(aryl)[4-aryl-1H-pyrrol-3-yl]methyl]-1H-imidazole, synthesis, anti-candida activity, and quantitative structure-analysis relationship studies. |
| AID631942 | Antileishmanial activity against Leishmania amazonensis MHOM/ BR/77/LTB0016 infected in CBA mouse assessed as development of cutaneous lesions at 50 mg/kg, po qd for 30 days administered 4 weeks post infection measured up to week 21 | 2011 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 21, Issue:24 | Synthesis and antileishmanial evaluation of 1-aryl-4-(4,5-dihydro-1H-imidazol-2-yl)-1H-pyrazole derivatives. |
| AID765651 | Antifungal activity against Saccharomyces cerevisiae assessed as growth inhibition at 0.5 mg/mL after 24 hrs by agar well diffusion assay | 2013 | European journal of medicinal chemistry, Sep, Volume: 67 | Synthesis of thiosemicarbazones derived from N-(4-hippuric acid)thiosemicarbazide and different carbonyl compounds as antimicrobial agents. |
| AID1171977 | Antibacterial activity against Proteus vulgaris MTCC 1771 assessed as zone of inhibition at 1 mg/disc after 24 hrs by disc diffusion method | 2015 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2 | Facile and diastereoselective synthesis of 3,2'-spiropyrrolidine-oxindoles derivatives, their molecular docking and antiproliferative activities. |
| AID1467465 | Antifungal activity against Aspergillus niger at 100 ug/ml after 48 hrs by agar well diffusion method | 2017 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 27, Issue:14 | Synthesis, SAR and molecular docking studies of benzo[d]thiazole-hydrazones as potential antibacterial and antifungal agents. |
| AID1472633 | Inhibition of CYP3A4 in human liver microsomes using midazolam as substrate upto 10 uM after 5 mins in presence of NADPH by LC-MS/MS analysis | 2018 | Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1 | Novel Terminal Bipheny-Based Diapophytoene Desaturases (CrtN) Inhibitors as Anti-MRSA/VISR/LRSA Agents with Reduced hERG Activity. |
| AID340965 | Antifungal activity against sKloeckera apiculata isolates from grapes by NCCLS M27-A2 method | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8 | Cross-resistance to medical and agricultural azole drugs in yeasts from the oropharynx of human immunodeficiency virus patients and from environmental Bavarian vine grapes. |
| AID456072 | Antifungal activity against Fulvia fulva TK 5318 after 72 hrs by serial dilution method | 2010 | Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1 | Novel 4-thiazolidinone derivatives as potential antifungal and antibacterial drugs. |
| AID479369 | Inhibition of human placental microsome CYP19 | 2010 | Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10 | Pharmacophore modeling strategies for the development of novel nonsteroidal inhibitors of human aromatase (CYP19). |
| AID492342 | Inhibition of human recombinant CYP24A1 expressed in chinese hamster V79 cells using [3H-1-beta]calcitriol after 60 mins by scintillation counting | 2010 | Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14 | Synthesis and CYP24A1 inhibitory activity of N-(2-(1H-imidazol-1-yl)-2-phenylethyl)arylamides. |
| AID606213 | Antifungal activity against Candida parapsilosis ATCC 0306392 by micro-broth dilution method | 2011 | European journal of medicinal chemistry, Jul, Volume: 46, Issue:7 | Design, synthesis and antifungal activities of novel 1,2,4-triazole derivatives. |
| AID377680 | Antifungal activity against Alternaria alternata after 48 hrs by NCCLS M27A method | 2006 | Journal of natural products, Jul, Volume: 69, Issue:7 | Phytochemistry and antifungal properties of the newly discovered tree Pleodendron costaricense. |
| AID554709 | Antimicrobial activity against Candida krusei NZCDC 89.221 after 48 hrs by liquid microdilution assay | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2 | Abc1p is a multidrug efflux transporter that tips the balance in favor of innate azole resistance in Candida krusei. |
| AID200311 | The compound was tested for antifungal activity against Saccharomyces cerevisiae MY1027 using agar dilution assay | 1987 | Journal of medicinal chemistry, Aug, Volume: 30, Issue:8 | Lysosomotropic agents. 7. Broad-spectrum antifungal activity of lysosomotropic detergents. |
| AID348960 | Antifungal activity against Trichophyton rubrum after 48 hrs by MTT assay | 2008 | European journal of medicinal chemistry, Jul, Volume: 43, Issue:7 | Synthesis and antimicrobial activities of 7-O-modified genistein derivatives. |
| AID488641 | Antimicrobial activity against Candida glabrata ATCC 30070 by broth dilution method | 2010 | Journal of natural products, Jun-25, Volume: 73, Issue:6 | Alkaloids from the bark of Guatteria hispida and their evaluation as antioxidant and antimicrobial agents. |
| AID245920 | Cytotoxicity to reduce human histolytic lymphoma U937 cells | 2004 | Journal of medicinal chemistry, Jul-29, Volume: 47, Issue:16 | Imidazole analogues of fluoxetine, a novel class of anti-Candida agents. |
| AID1103203 | Antifungal activity against Fusarium graminearum isolate CE169 after 48 to 72 hr | 2004 | Journal of agricultural and food chemistry, Jun-02, Volume: 52, Issue:11 | Antifungal chalcones and new caffeic acid esters from Zuccagnia punctata acting against soybean infecting fungi. |
| AID429371 | Antifungal activity against Aspergillus niger after 72 hrs by liquid dilution method | 2009 | European journal of medicinal chemistry, Aug, Volume: 44, Issue:8 | Mono and bis-6-arylbenzimidazo[1,2-c]quinazolines: a new class of antimicrobial agents. |
| AID214297 | In vitro antifungal activity against Trichophyton rubrum | 1984 | Journal of medicinal chemistry, Jul, Volume: 27, Issue:7 | Antimycotic azoles. 7. Synthesis and antifungal properties of a series of novel triazol-3-ones. |
| AID1217574 | Tmax in castrated pig plasma withdrawn from femoral vein at 200 mg/kg dosed via intrajejunal route by UPLC-tandem mass spectrometry | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5 | In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole. |
| AID1247100 | Antifungal activity against Aspergillus flavus after 48 to 72 hrs by two fold serial dilution method | 2015 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19 | Synthesis of BF₃ catalyzed Mannich derivatives with excellent ee from phenylpropanolamine, study of their antimicrobial activity and molecular docking. |
| AID454778 | Antifungal activity against Aspergillus fumigatus ATCC 26934 after 48 hrs by broth microdilution technique | 2009 | Bioorganic & medicinal chemistry, Nov-01, Volume: 17, Issue:21 | 5-Nitrofuranes and 5-nitrothiophenes with anti-Trypanosoma cruzi activity and ability to accumulate squalene. |
| AID530972 | Antifungal activity against Aspergillus fumigatus ATCC 90906 at 9.4 uM after 48 hrs by CLSI method | 2008 | Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7 | Potent in vitro antifungal activities of naturally occurring acetylenic acids. |
| AID1221960 | Apparent permeability from apical to basolateral side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY335979 | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2 | Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
| AID549052 | Antifungal activity against Candida albicans CA137 after 48 hrs by broth microdilution method | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | In vitro activities of retigeric acid B alone and in combination with azole antifungal agents against Candida albicans. |
| AID214425 | In vitro evaluation of minimum inhibitory concentration against Trichophyton rubrum 90 | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20 | Synthesis and antifungal activity of new azole derivatives containing an N-acylmorpholine ring. |
| AID285162 | Antimicrobial activity against non replicating persistence Mycobacterium tuberculosis H37Rv in anaerobic condition assessed as bacterial density after 10 days | 2007 | Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4 | Low-oxygen-recovery assay for high-throughput screening of compounds against nonreplicating Mycobacterium tuberculosis. |
| AID1196735 | Antifungal activity against Candida tropicalis NRLL Y 12968 after 48 hrs by broth microdilution assay | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | A novel series of thiazolyl-pyrazoline derivatives: synthesis and evaluation of antifungal activity, cytotoxicity and genotoxicity. |
| AID1075575 | Antimicrobial activity against Penicillium chrysogenum NRRL 1951 after 48 to 72 hrs by microbroth dilution method | 2014 | European journal of medicinal chemistry, Mar-03, Volume: 74 | Synthesis and biological evaluation of thiazoline derivatives as new antimicrobial and anticancer agents. |
| AID644192 | Antifungal activity against Aspergillus niger ATCC 6275 treated for 72 hrs followed by sub-cultivated for 5 days by serial dilution method | 2012 | Bioorganic & medicinal chemistry, Feb-15, Volume: 20, Issue:4 | Synthesis of novel sulfonamide-1,2,4-triazoles, 1,3,4-thiadiazoles and 1,3,4-oxadiazoles, as potential antibacterial and antifungal agents. Biological evaluation and conformational analysis studies. |
| AID243989 | In vitro inhibition against human placental cytochrome P450 17 expressed in Escherichia coli with 2.5 uM progesterone | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Synthesis and evaluation of imidazolylmethylenetetrahydronaphthalenes and imidazolylmethyleneindanes: potent inhibitors of aldosterone synthase. |
| AID623361 | Antifungal activity against Candida glabrata clinical isolate (Anadolu university) by NCCLS M27-A2 microbroth dilution method | 2011 | European journal of medicinal chemistry, Nov, Volume: 46, Issue:11 | Synthesis and anticandidal activity of new triazolothiadiazine derivatives. |
| AID49255 | Tested for minimum subinhibitory concentration against Candida albicans 4 (Candida albicans) at pH 6.5. | 1994 | Journal of medicinal chemistry, Jun-24, Volume: 37, Issue:13 | Derivatives of a novel cyclopeptolide. 1. Synthesis, antifungal activity, and structure-activity relationships. |
| AID7062 | Inhibitory activity against 5-lipoxygenase of RBL-1 cell line | 1992 | Journal of medicinal chemistry, Aug-21, Volume: 35, Issue:17 | Novel 1-(pyridylphenyl)-1-phenyl-2-imidazolylethanols with topical antiinflammatory activity. |
| AID429609 | Inhibition of 17-alpha-hydroxylase activity of rat testicular microsomal P450-17alpha | 2009 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 19, Issue:16 | Synthesis and biochemical evaluation of a range of sulfonated derivatives of 4-hydroxybenzyl imidazole as highly potent inhibitors of rat testicular 17alpha-hydroxylase/17,20-lyase (P-450(17alpha)). |
| AID1103209 | Antifungal activity against Alternaria alternata (CE172) after 48 to 72 hr | 2004 | Journal of agricultural and food chemistry, Jun-02, Volume: 52, Issue:11 | Antifungal chalcones and new caffeic acid esters from Zuccagnia punctata acting against soybean infecting fungi. |
| AID45503 | In vivo Evaluation of minimum inhibitory concentration against Candida albicans 60 | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20 | Synthesis and antifungal activity of new azole derivatives containing an N-acylmorpholine ring. |
| AID1229830 | Inhibition of human recombinant CYP3A4 assessed as remaining enzyme activity by measuring conversion of luciferin-PPXE into D-luciferin by luminescence CYP3A4 P450-Glo assay relative to untreated control | 2015 | Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13 | Design, synthesis, and anticonvulsant activity of new hybrid compounds derived from 2-(2,5-dioxopyrrolidin-1-yl)propanamides and 2-(2,5-dioxopyrrolidin-1-yl)butanamides. |
| AID575110 | Antifungal activity against Madurella mycetomatis isolate 45 by XTT assay | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Madurella mycetomatis is not susceptible to the echinocandin class of antifungal agents. |
| AID1196734 | Antifungal activity against Candida albicans ATCC 90028 after 48 hrs by broth microdilution assay | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | A novel series of thiazolyl-pyrazoline derivatives: synthesis and evaluation of antifungal activity, cytotoxicity and genotoxicity. |
| AID648381 | Antifungal activity against Malassezia pachydermatis after 48 to 72 hrs by twofold serial dilution method | 2012 | European journal of medicinal chemistry, May, Volume: 51 | Synthesis of novel spirooxindole derivatives by one pot multicomponent reaction and their antimicrobial activity. |
| AID150754 | Inhibition of P-glycoprotein, mouse L-mdr1b expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay | 2003 | Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9 | Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery. |
| AID456840 | Antifungal activity against Aspergillus fumigatus clinical isolate after 72 hrs by serial dilution method | 2010 | Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1 | Novel 4-thiazolidinone derivatives as potential antifungal and antibacterial drugs. |
| AID456691 | Antifungal activity against Candida albicans ATCC 10231 assessed as inhibition of fungal growth at 25 uM after 24 hrs by microbroth dilution method | 2010 | Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1 | New small-size peptides possessing antifungal activity. |
| AID496817 | Antimicrobial activity against Trypanosoma cruzi | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
| AID45330 | Evaluation of In vitro antifungal activity against Candida albicans C56 by broth macro dilution method | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20 | Synthesis and antifungal activity of new azole derivatives containing an N-acylmorpholine ring. |
| AID403692 | Antifungal activity against Candida albicans after 48 hrs by spectrophotometry | 2005 | Journal of natural products, Oct, Volume: 68, Issue:10 | Steroidal saponins from Smilax medica and their antifungal activity. |
| AID382514 | Antifungal activity against Candida glabrata isolate by broth dilution antifungal susceptibility test | 2008 | European journal of medicinal chemistry, Jan, Volume: 43, Issue:1 | New triazole and triazolothiadiazine derivatives as possible antimicrobial agents. |
| AID406957 | Antifungal activity against fluconazole-resistant Candida albicans isolated from oropharyngeal or vaginal disease patient after 48 hrs by broth microdilution test | 2008 | Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13 | 1-[(3-Aryloxy-3-aryl)propyl]-1H-imidazoles, new imidazoles with potent activity against Candida albicans and dermatophytes. Synthesis, structure-activity relationship, and molecular modeling studies. |
| AID635086 | Antifungal activity against Aspergillus niger NCIM 596 after 48 hrs by disk diffusion method | 2012 | European journal of medicinal chemistry, Jan, Volume: 47, Issue:1 | Synthesis, antimicrobial, antimycobacterial and structure-activity relationship of substituted pyrazolo-, isoxazolo-, pyrimido- and mercaptopyrimidocyclohepta[b]indoles. |
| AID600774 | Fungicidal activity against Aspergillus versicolor ATCC 11730 after 72 hrs | 2011 | Bioorganic & medicinal chemistry, May-15, Volume: 19, Issue:10 | Thiazole-based chalcones as potent antimicrobial agents. Synthesis and biological evaluation. |
| AID554720 | Antimicrobial activity against Saccharomyces cerevisiae isolate AD overexpressing Candida krusei ERG11C after 48 hrs by liquid microdilution assay | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2 | Abc1p is a multidrug efflux transporter that tips the balance in favor of innate azole resistance in Candida krusei. |
| AID1275149 | Antifungal activity against Aspergillus niger ATCC-1094 after 72 hrs by broth microdilution method | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Synthesis and biological evaluation of new naphthalene substituted thiosemicarbazone derivatives as potent antifungal and anticancer agents. |
| AID381184 | Antifungal activity against Candida parapsilosis after 24 to 72 hrs by disk diffusion method | 1999 | Journal of natural products, Sep, Volume: 62, Issue:9 | Antimicrobial and antitumor activities of mycosporulone. |
| AID551099 | Antifungal activity against Candida albicans by liquid dilution method | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1 | 3-[Benzimidazo- and 3-[benzothiadiazoleimidazo-(1,2-c)quinazolin-5-yl]-2H-chromene-2-ones as potent antimicrobial agents. |
| AID1221965 | Transporter substrate index of efflux ratio in human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY335979 | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2 | Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
| AID628508 | Antifungal activity against Fusarium solani at 200 ug/ml after 48 hrs by disc diffusion method | 2011 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21 | Synthesis and biological evaluation of some novel triazol-3-ones as antimicrobial agents. |
| AID1055305 | Antifungal activity against Candida albicans ATCC 10231 at 50 ug after 72 hrs by disk diffusion method | 2013 | European journal of medicinal chemistry, , Volume: 70 | Phosphorus-nitrogen compounds part 27. Syntheses, structural characterizations, antimicrobial and cytotoxic activities, and DNA interactions of new phosphazenes bearing secondary amino and pendant (4-fluorobenzyl)spiro groups. |
| AID1221966 | Ratio of plasma AUC in po dosed mdr1 knock out mouse to plasma AUC in po dosed wild type mouse | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2 | Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
| AID262709 | Inhibition of human placental CYP19 | 2006 | Journal of medicinal chemistry, Apr-06, Volume: 49, Issue:7 | Synthesis and evaluation of heteroaryl-substituted dihydronaphthalenes and indenes: potent and selective inhibitors of aldosterone synthase (CYP11B2) for the treatment of congestive heart failure and myocardial fibrosis. |
| AID551089 | Antifungal activity against Aspergillus niger at 1000 ug/mL after 72 hrs by agar diffusion assay | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1 | 3-[Benzimidazo- and 3-[benzothiadiazoleimidazo-(1,2-c)quinazolin-5-yl]-2H-chromene-2-ones as potent antimicrobial agents. |
| AID315653 | Inhibition of human CYP17 expressed in Escherichia coli co-expressed with NADPH-P450 reductase | 2008 | Bioorganic & medicinal chemistry, Feb-15, Volume: 16, Issue:4 | Synthesis, biological evaluation and molecular modelling studies of methyleneimidazole substituted biaryls as inhibitors of human 17alpha-hydroxylase-17,20-lyase (CYP17). Part I: Heterocyclic modifications of the core structure. |
| AID362917 | Antifungal activity against Sporobolomyces salmonicolor after 24 hrs by broth microdilution method | 2008 | Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17 | NO-donors. Part 17: Synthesis and antimicrobial activity of novel ketoconazole-NO-donor hybrid compounds. |
| AID648370 | Antifungal activity against Malassezia pachydermatis at 1000 ug/disc after 48 hrs by disc diffusion assay | 2012 | European journal of medicinal chemistry, May, Volume: 51 | Synthesis of novel spirooxindole derivatives by one pot multicomponent reaction and their antimicrobial activity. |
| AID628509 | Antifungal activity against Aspergillus niger at 100 ug/ml after 48 hrs by disc diffusion method | 2011 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21 | Synthesis and biological evaluation of some novel triazol-3-ones as antimicrobial agents. |
| AID1184068 | Inhibition of IDO1 (unknown origin) using L-tryptophan substrate incubated for 60 mins by HPLC | 2014 | European journal of medicinal chemistry, Sep-12, Volume: 84 | Detailed analysis and follow-up studies of a high-throughput screening for indoleamine 2,3-dioxygenase 1 (IDO1) inhibitors. |
| AID1130378 | Antifungal activity against Candida tropicalis assessed as growth inhibition in sabouraud broth after 14 days | 1979 | Journal of medicinal chemistry, Aug, Volume: 22, Issue:8 | Antimycotic imidazoles. part 4. Synthesis and antifungal activity of ketoconazole, a new potent orally active broad-spectrum antifungal agent. |
| AID380259 | Antifungal activity against Valsa mali by MTT assay | 2006 | Journal of natural products, Dec, Volume: 69, Issue:12 | Bioactive oligostilbenoids from the stem bark of Hopea exalata. |
| AID1473738 | Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1 | A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
| AID1130401 | Antifungal activity against Coccidioides immitis infected in mouse coccidioidomycosis model assessed as cell killing activity at 40 mg/kg, po od for 2.5 weeks relative to control | 1979 | Journal of medicinal chemistry, Aug, Volume: 22, Issue:8 | Antimycotic imidazoles. part 4. Synthesis and antifungal activity of ketoconazole, a new potent orally active broad-spectrum antifungal agent. |
| AID519285 | Antifungal activity against Candida parapsilosis ATCC 22019 by CLSI M27-A2 microdilution method | 2008 | Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3 | Reliability of the WIDERYST susceptibility testing system for detection of in vitro antifungal resistance in yeasts. |
| AID84882 | Percentage increase of the total serum cholesterol in male hamsters at a dose of 25 mg/dL orally administered for 14 days | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | Selective inhibition of mammalian lanosterol 14 alpha-demethylase: a possible strategy for cholesterol lowering. |
| AID1168629 | Antimicrobial activity against Candida albicans ATCC 10231 at 50 ug after 18 hrs by agar well diffusion assay | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | Phosphorus-nitrogen compounds. Part 29. Syntheses, crystal structures, spectroscopic and stereogenic properties, electrochemical investigations, antituberculosis, antimicrobial and cytotoxic activities and DNA interactions of ansa-spiro-ansa cyclotetrapho |
| AID311905 | Antifeedant activity against Spodoptera littoralis larvae at 10 ug/disk by disk-choice assay | 2007 | Journal of natural products, Dec, Volume: 70, Issue:12 | Bioactive polychlorinated bibenzyls from the liverwort Riccardia polyclada. |
| AID404304 | Effect on human MRP2-mediated estradiol-17-beta-glucuronide transport in Sf9 cells inverted membrane vesicles relative to control | 2008 | Journal of medicinal chemistry, Jun-12, Volume: 51, Issue:11 | Prediction and identification of drug interactions with the human ATP-binding cassette transporter multidrug-resistance associated protein 2 (MRP2; ABCC2). |
| AID425717 | Antimicrobial activity against Balamuthia mandrillaris ATCC 50209 infected in HBMEC assessed as inhibition of encystment at 10 ug/mL after 7 days | 2007 | Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12 | Effect of antimicrobial compounds on Balamuthia mandrillaris encystment and human brain microvascular endothelial cell cytopathogenicity. |
| AID420079 | Antifungal activity against Cryptococcus neoformans CAP67 after 48 hrs by broth microdilution assay | 2009 | Bioorganic & medicinal chemistry, Jun-01, Volume: 17, Issue:11 | Bulky 1,4-benzoxazine derivatives with antifungal activity. |
| AID318316 | Inhibition of human CYP3A4 | 2008 | Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7 | Design, synthesis, and biological evaluation of (hydroxyphenyl)naphthalene and -quinoline derivatives: potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1) for the treatment of estrogen-dependent disease |
| AID1472786 | Inhibition of CYP3A4 (unknown origin) expressed in baculosomes | 2018 | Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3 | Comprehensive Synthesis of Amino Acid-Derived Thiazole Peptidomimetic Analogues to Understand the Enigmatic Drug/Substrate-Binding Site of P-Glycoprotein. |
| AID201546 | In vitro antifungal activity against Saprolegnia sp | 1984 | Journal of medicinal chemistry, Jul, Volume: 27, Issue:7 | Antimycotic azoles. 7. Synthesis and antifungal properties of a series of novel triazol-3-ones. |
| AID39702 | In vitro antifungal activity against human pathogenic fungi, Aspergillus fumigatus | 2000 | Bioorganic & medicinal chemistry letters, Apr-17, Volume: 10, Issue:8 | Suitably functionalised pyrimidines as potential antimycotic agents. |
| AID554707 | Antimicrobial activity against Candida krusei NZCDC 89.021 after 48 hrs by liquid microdilution assay | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2 | Abc1p is a multidrug efflux transporter that tips the balance in favor of innate azole resistance in Candida krusei. |
| AID1075576 | Antimicrobial activity against Aspergillus parasiticus NRRL 465 after 48 to 72 hrs by microbroth dilution method | 2014 | European journal of medicinal chemistry, Mar-03, Volume: 74 | Synthesis and biological evaluation of thiazoline derivatives as new antimicrobial and anticancer agents. |
| AID1110735 | Antifungal activity against Aspergillus fumigatus 231 after 24 hr by microdilution broth method | 2002 | Farmaco (Societa chimica italiana : 1989), Feb, Volume: 57, Issue:2 | Ring substituted 3-phenyl-1-(2-pyrazinyl)-2-propen-1-ones as potential photosynthesis-inhibiting, antifungal and antimycobacterial agents. |
| AID242735 | In vitro inhibitory concentration against human placental CYP19 incubated with 500 nM of substrate androstenedione in presence of the compound; nd is not determined | 2005 | Journal of medicinal chemistry, Mar-10, Volume: 48, Issue:5 | Synthesis and evaluation of (pyridylmethylene)tetrahydronaphthalenes/-indanes and structurally modified derivatives: potent and selective inhibitors of aldosterone synthase. |
| AID456068 | Antifungal activity against Aspergillus versicolor ATCC 11730 after 72 hrs by serial dilution method | 2010 | Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1 | Novel 4-thiazolidinone derivatives as potential antifungal and antibacterial drugs. |
| AID575104 | Antifungal activity against Madurella mycetomatis isolate 31 by XTT assay | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Madurella mycetomatis is not susceptible to the echinocandin class of antifungal agents. |
| AID150756 | Inhibition of P-gp was determined using rhodamine-assay in human CaCo-2 cells | 2003 | Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9 | Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery. |
| AID1179276 | Antimicrobial activity against Malassezia pachydermatis at 1 mg/disc after 24 hrs by disc diffusion assay | 2014 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 24, Issue:14 | Synthesis, antimicrobial and molecular docking studies of enantiomerically pure N-alkylated β-amino alcohols from phenylpropanolamines. |
| AID623358 | Antifungal activity against Candida parapsilosis NRRL Y-12696 by NCCLS M27-A2 microbroth dilution method | 2011 | European journal of medicinal chemistry, Nov, Volume: 46, Issue:11 | Synthesis and anticandidal activity of new triazolothiadiazine derivatives. |
| AID549050 | Antifungal activity against Candida albicans CA10 after 48 hrs by broth microdilution method | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | In vitro activities of retigeric acid B alone and in combination with azole antifungal agents against Candida albicans. |
| AID83865 | Effect on total serum cholesterol in male hamsters at a dose of 50 mg/kg orally administered for 14 days | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | Selective inhibition of mammalian lanosterol 14 alpha-demethylase: a possible strategy for cholesterol lowering. |
| AID161641 | Inhibition of Progesterone 21-hydroxylase cytochrome P450 21 | 1992 | Journal of medicinal chemistry, Jul-24, Volume: 35, Issue:15 | Stereoisomers of ketoconazole: preparation and biological activity. |
| AID362165 | Inhibition of human CYP11B1 expressed in hamster V79MZh11B1 cells | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16 | Synthesis, biological evaluation, and molecular modeling of abiraterone analogues: novel CYP17 inhibitors for the treatment of prostate cancer. |
| AID631944 | Toxicity in CBA mouse infected with Leishmania amazonensis MHOM/ BR/77/LTB0016 assessed as weight loss at 50 mg/kg, po qd for 30 days administered 4 week post infection measured up to week 21 | 2011 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 21, Issue:24 | Synthesis and antileishmanial evaluation of 1-aryl-4-(4,5-dihydro-1H-imidazol-2-yl)-1H-pyrazole derivatives. |
| AID315662 | Inhibition of recombinant CYP2C19 at 10 uM | 2008 | Bioorganic & medicinal chemistry, Feb-15, Volume: 16, Issue:4 | Synthesis, biological evaluation and molecular modelling studies of methyleneimidazole substituted biaryls as inhibitors of human 17alpha-hydroxylase-17,20-lyase (CYP17). Part I: Heterocyclic modifications of the core structure. |
| AID447229 | Antifungal activity against Debaryomyces hansenii DSM 70238 at 20 ug after 72 hrs by agar disk diffusion assay | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11 | Synthesis, Raman, FT-IR, NMR spectroscopic characterization, antimicrobial activity, cytotoxicity and DNA binding of new mixed aza-oxo-thia macrocyclic compounds. |
| AID376053 | Antifungal activity against Aspergillus fumigatus ATCC 26934 by agar dilution method | 1999 | Journal of natural products, Oct, Volume: 62, Issue:10 | In vitro evaluation of antifungal properties of phenylpropanoids and related compounds acting against dermatophytes. |
| AID255299 | Percent inhibition against recombinant human cytochrome P450 17A1 using progesterone | 2005 | Journal of medicinal chemistry, Oct-20, Volume: 48, Issue:21 | Heteroaryl-substituted naphthalenes and structurally modified derivatives: selective inhibitors of CYP11B2 for the treatment of congestive heart failure and myocardial fibrosis. |
| AID1334864 | Inhibition of CYP3A4 in human liver microsomes assessed as reduction in nifedipine oxidation incubated for 10 mins | 2017 | Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2 | Discovery of biphenyl imidazole derivatives as potent antifungal agents: Design, synthesis, and structure-activity relationship studies. |
| AID362818 | Antifungal activity against Fusarium solani after 48 hrs by microdilution susceptibility method | 2008 | European journal of medicinal chemistry, May, Volume: 43, Issue:5 | Synthesis and antimicrobial activity of novel sulfone-linked bis heterocycles. |
| AID249259 | Minimum inhibitory concentration to inhibit 50% of the isolates | 2004 | Journal of medicinal chemistry, Jul-29, Volume: 47, Issue:16 | Imidazole analogues of fluoxetine, a novel class of anti-Candida agents. |
| AID636992 | Antifungal activity against Aspergillus clavatus after 48 hrs by agar streak dilution method | 2012 | European journal of medicinal chemistry, Feb, Volume: 48 | Synthesis and biological evaluation of some thiazolidinones as antimicrobial agents. |
| AID197814 | In vitro evaluation of minimum inhibitory concentration against Rhodotorula rubra 16 | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20 | Synthesis and antifungal activity of new azole derivatives containing an N-acylmorpholine ring. |
| AID341133 | Antifungal activity against sSaccharomyces cerevisiae isolates from grapes by NCCLS M27-A2 method | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8 | Cross-resistance to medical and agricultural azole drugs in yeasts from the oropharynx of human immunodeficiency virus patients and from environmental Bavarian vine grapes. |
| AID334244 | Antimicrobial activity against Bacillus subtilis NCTC 10073 after 24 hrs by microdilution technique | 2002 | Journal of natural products, Apr, Volume: 65, Issue:4 | Antimicrobial activities of a new schizozygane indoline alkaloid from Schizozygia coffaeoides and the revised structure of isoschizogaline. |
| AID405019 | Antifungal activity against Sporothrix schenckii P20825 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by Sensititre YeastOne method | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods. |
| AID594133 | Antimicrobial activity against Klebsiella pneumoniae ATCC 13883 after 24 hrs by agar well diffusion method | 2011 | European journal of medicinal chemistry, May, Volume: 46, Issue:5 | Synthesis, antimicrobial, antioxidant, anti-hemolytic and cytotoxic evaluation of new imidazole-based heterocycles. |
| AID688646 | Fungicidal activity against Aspergillus niger after 48 hrs by broth dilution method | 2011 | European journal of medicinal chemistry, Nov, Volume: 46, Issue:11 | Synthesis and antimicrobial activity of amido linked pyrrolyl and pyrazolyl-oxazoles, thiazoles and imidazoles. |
| AID1450075 | Inhibition of recombinant human CYP3A4 expressed in insect cells at >= 1 uM using DBOMF as substrate pretreated for 10 mins followed by substrate addition measured every minute for 15 mins in presence of NADP+ by fluorescence assay relative to control | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11 | Cytochrome P450 binding studies of novel tacrine derivatives: Predicting the risk of hepatotoxicity. |
| AID554712 | Antimicrobial activity against Candida krusei IFO0011 after 48 hrs by CLSI method | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2 | Abc1p is a multidrug efflux transporter that tips the balance in favor of innate azole resistance in Candida krusei. |
| AID1229829 | Inhibition of human recombinant CYP3A4 assessed as remaining enzyme activity by measuring conversion of luciferin-PPXE into D-luciferin at 100 uM by luminescence CYP3A4 P450-Glo assay relative to untreated control | 2015 | Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13 | Design, synthesis, and anticonvulsant activity of new hybrid compounds derived from 2-(2,5-dioxopyrrolidin-1-yl)propanamides and 2-(2,5-dioxopyrrolidin-1-yl)butanamides. |
| AID42875 | Inhibition of Candida krusei ATCC 6258 growth for 48 hours in vitro. | 2001 | Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17 | 3-Phenyl-5-acyloxymethyl-2H,5H-furan-2-ones: synthesis and biological activity of a novel group of potential antifungal drugs. |
| AID1217571 | Cmax in castrated pig plasma withdrawn from portal vein at 200 mg/kg dosed via intrajejunal route by UPLC-tandem mass spectrometry | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5 | In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole. |
| AID574259 | Antifungal activity against 24 hrs cultures of 10'7 cells/ml Candida albicans ATCC 90028 planktonic cells by XTT reduction method | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | Cell density and cell aging as factors modulating antifungal resistance of Candida albicans biofilms. |
| AID1221964 | Transporter substrate index ratio of permeability from basolateral to apical side in human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY335979 | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2 | Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
| AID449686 | Antifungal activity against Curvularia lunata NCIM 716 at 100 ug/disk after 48 hrs by agar disk diffusion method | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11 | Synthesis, antimicrobial and antioxidant activities of substituted pyrazoles, isoxazoles, pyrimidine and thioxopyrimidine derivatives. |
| AID1130394 | Antifungal activity against Candida albicans B2630 infected in ovariectomized and hysterectomized Wistar rat vaginal candidosis model at 2.5 mg/kg, po for 14 days by prophylactic treatment | 1979 | Journal of medicinal chemistry, Aug, Volume: 22, Issue:8 | Antimycotic imidazoles. part 4. Synthesis and antifungal activity of ketoconazole, a new potent orally active broad-spectrum antifungal agent. |
| AID625276 | FDA Liver Toxicity Knowledge Base Benchmark Dataset (LTKB-BD) drugs of most concern for DILI | 2011 | Drug discovery today, Aug, Volume: 16, Issue:15-16 | FDA-approved drug labeling for the study of drug-induced liver injury. |
| AID262550 | Antifungal activity against Aspergillus fumigatus | 2006 | Journal of medicinal chemistry, Apr-20, Volume: 49, Issue:8 | Structure-based optimization of azole antifungal agents by CoMFA, CoMSIA, and molecular docking. |
| AID1171984 | Antifungal activity against Candida albicans MTCC 227 assessed as zone of inhibition at 1 mg/disc after 48 hrs by disc diffusion method | 2015 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2 | Facile and diastereoselective synthesis of 3,2'-spiropyrrolidine-oxindoles derivatives, their molecular docking and antiproliferative activities. |
| AID53228 | Tested for inhibitory activity against Cytochrome P450 17 from rat testicular microsomes | 2000 | Journal of medicinal chemistry, Nov-16, Volume: 43, Issue:23 | Synthesis and evaluation of 17-aliphatic heterocycle-substituted steroidal inhibitors of 17alpha-hydroxylase/C17-20-lyase (P450 17). |
| AID49973 | In vitro minimum inhibitory concentration of compound was determined against Candida glabrata after 24 hr r | 2000 | Bioorganic & medicinal chemistry letters, Aug-21, Volume: 10, Issue:16 | 3-Phenyl-5-methyl-2H,5H-furan-2-ones: tuning antifungal activity by varying substituents on the phenyl ring. |
| AID494007 | Antifungal activity against Cryptococcus neoformans ATCC 32264 assessed as inhibition of fungal growth at 12.5 uM | 2010 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 20, Issue:16 | New antifungal peptides. Synthesis, bioassays and initial structure prediction by CD spectroscopy. |
| AID490137 | Antifungal activity against Trichophyton rubrum ATCC 10218 after 24 hrs by MTT assay | 2010 | European journal of medicinal chemistry, Jul, Volume: 45, Issue:7 | Synthesis of some N-alkyl substituted urea derivatives as antibacterial and antifungal agents. |
| AID1301011 | Inhibition of human recombinant CYP2D6 using MFC as substrate incubated for 40 mins by fluorimetry | 2016 | European journal of medicinal chemistry, Jul-19, Volume: 117 | 2-hydroxyisoquinoline-1,3(2H,4H)-diones (HIDs) as human immunodeficiency virus type 1 integrase inhibitors: Influence of the alkylcarboxamide substitution of position 4. |
| AID554721 | Antimicrobial activity against Saccharomyces cerevisiae isolate ADdelta overexpressing Candida krusei ERG11g after 48 hrs by liquid microdilution assay | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2 | Abc1p is a multidrug efflux transporter that tips the balance in favor of innate azole resistance in Candida krusei. |
| AID48795 | In vitro minimum inhibitory concentration of compound was determined against Candida tropicalis after 24 hr r | 2000 | Bioorganic & medicinal chemistry letters, Aug-21, Volume: 10, Issue:16 | 3-Phenyl-5-methyl-2H,5H-furan-2-ones: tuning antifungal activity by varying substituents on the phenyl ring. |
| AID1110747 | Antifungal activity against Candida albicans ATCC 44859 after 24 hr by microdilution broth method | 2002 | Farmaco (Societa chimica italiana : 1989), Feb, Volume: 57, Issue:2 | Ring substituted 3-phenyl-1-(2-pyrazinyl)-2-propen-1-ones as potential photosynthesis-inhibiting, antifungal and antimycobacterial agents. |
| AID405112 | Antimicrobial activity against Cunninghamella sp. assessed as percent of susceptible isolates after 24 hrs | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | In vitro susceptibilities of 217 clinical isolates of zygomycetes to conventional and new antifungal agents. |
| AID1179275 | Antimicrobial activity against Candida albicans MTCC 227 at 1 mg/disc after 24 hrs by disc diffusion assay | 2014 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 24, Issue:14 | Synthesis, antimicrobial and molecular docking studies of enantiomerically pure N-alkylated β-amino alcohols from phenylpropanolamines. |
| AID255339 | Percent inhibition against human cytochrome P450 11B2 expressed in fission yeast, incubated with [14C]deoxycorticosterone | 2005 | Journal of medicinal chemistry, Oct-20, Volume: 48, Issue:21 | Heteroaryl-substituted naphthalenes and structurally modified derivatives: selective inhibitors of CYP11B2 for the treatment of congestive heart failure and myocardial fibrosis. |
| AID362912 | Antifungal activity against Fusarium oxysporum after 24 hrs by broth microdilution method | 2008 | Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17 | NO-donors. Part 17: Synthesis and antimicrobial activity of novel ketoconazole-NO-donor hybrid compounds. |
| AID600768 | Antifungal activity against Aspergillus fumigatus plant isolate after 72 hrs by serial dilution method | 2011 | Bioorganic & medicinal chemistry, May-15, Volume: 19, Issue:10 | Thiazole-based chalcones as potent antimicrobial agents. Synthesis and biological evaluation. |
| AID491986 | Inhibition of human CYP11B2 expressed in hamster V79MZh cells | 2010 | Journal of medicinal chemistry, Jul-08, Volume: 53, Issue:13 | Isopropylidene substitution increases activity and selectivity of biphenylmethylene 4-pyridine type CYP17 inhibitors. |
| AID48275 | Tested In vitro for antifungal activity against candida Spp (Candida glabrata, Candida krusei) at pH 5.8 | 2002 | Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13 | Antifungal agents. 10. New derivatives of 1-[(aryl)[4-aryl-1H-pyrrol-3-yl]methyl]-1H-imidazole, synthesis, anti-candida activity, and quantitative structure-analysis relationship studies. |
| AID1429861 | n-octanol-phosphate buffer distribution coefficient, log D of the compound at pH 2 after 90 mins by shake-flask method | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Crystal structures, binding interactions, and ADME evaluation of brain penetrant N-substituted indazole-5-carboxamides as subnanomolar, selective monoamine oxidase B and dual MAO-A/B inhibitors. |
| AID1435416 | Anti-bacterial activity against Bacillus subtilis ATCC 33712 measured after 24 hrs by microtiter broth dilution method | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Design, synthesis and antimicrobial evaluation of novel benzoxazole derivatives. |
| AID1157296 | Antifungal activity against Trichophyton rubrum Cmccftla assessed as growth inhibition by automatic microplate reader analysis | 2014 | Journal of natural products, May-23, Volume: 77, Issue:5 | Polyhydroxy cyclohexanols from a Dendrodochium sp. fungus associated with the sea cucumber Holothuria nobilis Selenka. |
| AID54783 | Inhibition of recombinant human Cytochrome P450 3A4 with BFC [7-benzyloxy-4-trifluoromethylcoumarin] after 5 minutes | 2003 | Journal of medicinal chemistry, Aug-28, Volume: 46, Issue:18 | Fluorine substitution can block CYP3A4 metabolism-dependent inhibition: identification of (S)-N-[1-(4-fluoro-3- morpholin-4-ylphenyl)ethyl]-3- (4-fluorophenyl)acrylamide as an orally bioavailable KCNQ2 opener devoid of CYP3A4 metabolism-dependent inhibiti |
| AID287718 | Ratio of IC50 for human THP1 cells to IC50 for Trypanosoma cruzi CL Brener epimastigotes | 2007 | Bioorganic & medicinal chemistry, Apr-01, Volume: 15, Issue:7 | Second generation of 5-ethenylbenzofuroxan derivatives as inhibitors of Trypanosoma cruzi growth: synthesis, biological evaluation, and structure-activity relationships. |
| AID1164256 | Inhibition of human recombinant CYP3A4 incubated for 5 mins by fluorescence assay | 2014 | ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9 | Exploration of 3-Aminoazetidines as Triple Reuptake Inhibitors by Bioisosteric Modification of 3-α-Oxyazetidine. |
| AID48265 | Tested In vitro for antifungal activity against candida Spp (Candida glabrata, Candida krusei) at pH 5.8 | 2002 | Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13 | Antifungal agents. 10. New derivatives of 1-[(aryl)[4-aryl-1H-pyrrol-3-yl]methyl]-1H-imidazole, synthesis, anti-candida activity, and quantitative structure-analysis relationship studies. |
| AID554719 | Antimicrobial activity against Saccharomyces cerevisiae isolate ADdelta overexpressing Candida albicans ERG11A after 48 hrs by liquid microdilution assay | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2 | Abc1p is a multidrug efflux transporter that tips the balance in favor of innate azole resistance in Candida krusei. |
| AID588213 | Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents | 2010 | Chemical research in toxicology, Jan, Volume: 23, Issue:1 | Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species. |
| AID262548 | Antifungal activity against Candida tropicalis | 2006 | Journal of medicinal chemistry, Apr-20, Volume: 49, Issue:8 | Structure-based optimization of azole antifungal agents by CoMFA, CoMSIA, and molecular docking. |
| AID1217570 | AUC (0 to 6 hrs) in castrated pig plasma withdrawn from femoral vein at 200 mg/kg dosed via intrajejunal route by UPLC-tandem mass spectrometry | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5 | In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole. |
| AID1319283 | Inhibition of CYP3A4 in human liver microsomes using midazolam as substrate assessed as reduction in 1-OH-midazolam formation by LC/MS/MS analysis | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18 | Identification of (R)-(2-Chloro-3-(trifluoromethyl)phenyl)(1-(5-fluoropyridin-2-yl)-4-methyl-6,7-dihydro-1H-imidazo[4,5-c]pyridin-5(4H)-yl)methanone (JNJ 54166060), a Small Molecule Antagonist of the P2X7 receptor. |
| AID530576 | Antileishmanial activity against GFP-tagged at NH2 terminus Leishmania infantum promastigotes overexpressing LiABCG6 assessed as cell viability after 72 hrs by MTT assay | 2008 | Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10 | Characterization of an ABCG-like transporter from the protozoan parasite Leishmania with a role in drug resistance and transbilayer lipid movement. |
| AID47888 | Evaluation of In vitro antifungal activity against Candida parapsilosis ATCC 22019 by broth macro dilution method | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20 | Synthesis and antifungal activity of new azole derivatives containing an N-acylmorpholine ring. |
| AID582798 | Antifungal activity against Candida albicans isolate 177 by broth dilution method | 2010 | Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11 | Identification and characterization of four azole-resistant erg3 mutants of Candida albicans. |
| AID1209489 | Antagonist activity at rat PXR expressed in human HepG2 cells coexpressing CYP3A4 assessed as inhibition of PCN-induced receptor activation at 30 uM after 24 hrs by dual luciferase reporter gene assay | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1 | Species-dependent and receptor-selective action of bilobalide on the function of constitutive androstane receptor and pregnane X receptor. |
| AID1281964 | Inhibition of recombinant human CYP3A4 by luminescence -based microplate reader assay | 2016 | European journal of medicinal chemistry, Apr-13, Volume: 112 | Rational design in search for 5-phenylhydantoin selective 5-HT7R antagonists. Molecular modeling, synthesis and biological evaluation. |
| AID1079943 | Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source] | |||
| AID377672 | Antifungal activity against wild type Candida albicans Al-1 after 48 hrs by NCCLS M27A method | 2006 | Journal of natural products, Jul, Volume: 69, Issue:7 | Phytochemistry and antifungal properties of the newly discovered tree Pleodendron costaricense. |
| AID48456 | Tested in vitro for antifungal activity against candida Spp (Candida glabrata, Candida krusei) at pH 7.2 (percent of resistant species at 256 ug/mL) | 2002 | Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13 | Antifungal agents. 10. New derivatives of 1-[(aryl)[4-aryl-1H-pyrrol-3-yl]methyl]-1H-imidazole, synthesis, anti-candida activity, and quantitative structure-analysis relationship studies. |
| AID554711 | Antimicrobial activity against Candida krusei B2399 after 48 hrs by CLSI method | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2 | Abc1p is a multidrug efflux transporter that tips the balance in favor of innate azole resistance in Candida krusei. |
| AID554723 | Fold resistant, ratio of MIC for Saccharomyces cerevisiae isolate ADdelta overexpressing Candida albicans ERG11A to MIC for Saccharomyces cerevisiae isolate ADdelta overexpressing Abc1p | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2 | Abc1p is a multidrug efflux transporter that tips the balance in favor of innate azole resistance in Candida krusei. |
| AID555133 | Antimicrobial activity against Candida glabrata by EUCAST broth microdilution method | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Fenticonazole activity measured by the methods of the European Committee on Antimicrobial Susceptibility Testing and CLSI against 260 Candida vulvovaginitis isolates from two European regions and annotations on the prevalent genotypes. |
| AID532570 | Antifungal activity against wild-type Candida glabrata isolate 21231 by Etest method | 2008 | Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10 | A nonsense mutation in the ERG6 gene leads to reduced susceptibility to polyenes in a clinical isolate of Candida glabrata. |
| AID574248 | Antifungal activity against 10'7 cells/ml Candida albicans ATCC 90028 planktonic cells by XTT reduction assay | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | Cell density and cell aging as factors modulating antifungal resistance of Candida albicans biofilms. |
| AID1055880 | Inhibition of Wistar rat testicular C17,20-lyase using [3H]17-hydroxyprogesterone as substrate preincubated for 20 mins | 2013 | European journal of medicinal chemistry, , Volume: 70 | An efficient approach to novel 17-5'-(1',2',4')-oxadiazolyl androstenes via the cyclodehydration of cytotoxic O-steroidacylamidoximes, and an evaluation of their inhibitory action on 17α-hydroxylase/C₁₇,₂₀-lyase. |
| AID1075570 | Antimicrobial activity against wild type Fusarium culmorum after 48 to 72 hrs by microbroth dilution method | 2014 | European journal of medicinal chemistry, Mar-03, Volume: 74 | Synthesis and biological evaluation of thiazoline derivatives as new antimicrobial and anticancer agents. |
| AID407019 | Antimicrobial activity against Chk1 deficient Candida albicans CHK21 at planktonic cell density of 10'8 cells/ml after 48 hrs by XTT assay | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | Role for cell density in antifungal drug resistance in Candida albicans biofilms. |
| AID537733 | Binding affinity to Candida albicans CaCdr1p expressed in yeast AD1-8u | 2010 | European journal of medicinal chemistry, Nov, Volume: 45, Issue:11 | Analysis of physico-chemical properties of substrates of ABC and MFS multidrug transporters of pathogenic Candida albicans. |
| AID456067 | Antifungal activity against Aspergillus niger ATCC 6275 after 72 hrs by serial sub-cultivation method | 2010 | Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1 | Novel 4-thiazolidinone derivatives as potential antifungal and antibacterial drugs. |
| AID47868 | Evaluation of In vitro antifungal activity against Candida parapsilosis C74 by broth macro dilution method | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20 | Synthesis and antifungal activity of new azole derivatives containing an N-acylmorpholine ring. |
| AID303379 | Antitrypanosomal activity against Trypanosoma cruzi CL Brener | 2007 | Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24 | In vivo anti-Chagas vinylthio-, vinylsulfinyl-, and vinylsulfonylbenzofuroxan derivatives. |
| AID1557079 | Antifungal activity against Candida glabrata ATCC 2001 assessed as reduction in fungal cell growth incubated for 24 hrs by MTT based broth double dilution method | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Antifungal activity, mode of action variability, and subcellular distribution of coumarin-based antifungal azoles. |
| AID52776 | Compound was tested for the inhibition of Chymotrypsinogen | 2003 | Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21 | Identification and prediction of promiscuous aggregating inhibitors among known drugs. |
| AID723707 | Fungicidal activity against Penicillium funiculosum ATCC 36839 after 72 hrs by serial subcultivation method | 2013 | Bioorganic & medicinal chemistry, Jan-15, Volume: 21, Issue:2 | Synthesis and biological evaluation of some 5-arylidene-2-(1,3-thiazol-2-ylimino)-1,3-thiazolidin-4-ones as dual anti-inflammatory/antimicrobial agents. |
| AID244787 | Antifungal activity to inhibit Candida parapsilosis ATCC 22019 | 2004 | Journal of medicinal chemistry, Jul-29, Volume: 47, Issue:16 | Imidazole analogues of fluoxetine, a novel class of anti-Candida agents. |
| AID723706 | Antifungal activity against Aspergillus flavus ATCC 9643 after 72 hrs by serial dilution technique | 2013 | Bioorganic & medicinal chemistry, Jan-15, Volume: 21, Issue:2 | Synthesis and biological evaluation of some 5-arylidene-2-(1,3-thiazol-2-ylimino)-1,3-thiazolidin-4-ones as dual anti-inflammatory/antimicrobial agents. |
| AID494008 | Antifungal activity against Cryptococcus neoformans ATCC 32264 assessed as inhibition of fungal growth at 6.25 uM | 2010 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 20, Issue:16 | New antifungal peptides. Synthesis, bioassays and initial structure prediction by CD spectroscopy. |
| AID53371 | Inhibition of human testicular 17-alpha-hydroxylase | 1996 | Journal of medicinal chemistry, Oct-11, Volume: 39, Issue:21 | Synthesis and evaluation of pregnane derivatives as inhibitors of human testicular 17 alpha-hydroxylase/C17,20-lyase. |
| AID37847 | Inhibition of Aspergillus fumigatus 231 growth for 24 hours in vitro. | 2001 | Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17 | 3-Phenyl-5-acyloxymethyl-2H,5H-furan-2-ones: synthesis and biological activity of a novel group of potential antifungal drugs. |
| AID363728 | Antimicrobial activity against Candida albicans C126 isolate at 6.25 ug/ml after 24 hrs | 2008 | Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17 | In vitro antifungal activity of polyfunctionalized 2-(hetero)arylquinolines prepared through imino Diels-Alder reactions. |
| AID405028 | Antifungal activity against Sporothrix schenckii MRSS4 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by Sensititre YeastOne method | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods. |
| AID45341 | In vitro Minimum inhibitory concentration was determined by microbroth dilution assay on Candida albicans | 1992 | Journal of medicinal chemistry, Jan, Volume: 35, Issue:1 | Synthesis, specificity, and antifungal activity of inhibitors of the Candida albicans delta 24-sterol methyltransferase. |
| AID481667 | Antifungal activity against Candida albicans NRRL Y-12983 after 24 hrs by broth microdilution assay | 2010 | European journal of medicinal chemistry, May, Volume: 45, Issue:5 | Synthesis and the selective antifungal activity of 5,6,7,8-tetrahydroimidazo[1,2-a]pyridine derivatives. |
| AID524796 | Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay | 2009 | Nature chemical biology, Oct, Volume: 5, Issue:10 | Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum. |
| AID284091 | Antifungal activity against Candida albicans C130-2000 after 48 hrs | 2007 | Bioorganic & medicinal chemistry, Jan-01, Volume: 15, Issue:1 | Synthesis and antifungal activity of (Z)-5-arylidenerhodanines. |
| AID403693 | Antifungal activity against Candida glabrata after 48 hrs by spectrophotometry | 2005 | Journal of natural products, Oct, Volume: 68, Issue:10 | Steroidal saponins from Smilax medica and their antifungal activity. |
| AID572696 | Binding affinity to Mycobacterium smegmatis ATCC 700084 CYP164A2 in presence of 0.5 M NaCl at pH7.5 | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | Identification, characterization, and azole-binding properties of Mycobacterium smegmatis CYP164A2, a homolog of ML2088, the sole cytochrome P450 gene of Mycobacterium leprae. |
| AID1184075 | Inhibition of IDO1 (unknown origin) at highest soluble concentration using L-tryptophan substrate incubated for 60 mins by HPLC | 2014 | European journal of medicinal chemistry, Sep-12, Volume: 84 | Detailed analysis and follow-up studies of a high-throughput screening for indoleamine 2,3-dioxygenase 1 (IDO1) inhibitors. |
| AID1464255 | Inhibition of N-terminal MBP-tagged human CYP24A1 expressed in Escherichia coli assessed as reduction in hydrolase activity incubated for 25 mins using Adx, AdR and 1,25(OH)2D3 | 2017 | Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20 | Analysis of the binding sites of vitamin D 1α-hydroxylase (CYP27B1) and vitamin D 24-hydroxylase (CYP24A1) for the design of selective CYP24A1 inhibitors: Homology modelling, molecular dynamics simulations and identification of key binding requirements. |
| AID211160 | Minimum inhibitory concentration against Trichophyton ajelloi | 2004 | Bioorganic & medicinal chemistry letters, Feb-09, Volume: 14, Issue:3 | Synthesis and antifungal activities of phenylenedithioureas. |
| AID566947 | Antifungal activity against Candida albicans ATCC 10231 assessed as inhibition of fungal growth at 200 uM after 24 hrs by microplate analysis | 2011 | European journal of medicinal chemistry, Jan, Volume: 46, Issue:1 | Penetratin analogues acting as antifungal agents. |
| AID687500 | Antifungal activity against Candida albicans ATCC 10231 after 48 hrs by NCCLS broth microdilution method | 2012 | Bioorganic & medicinal chemistry, Oct-15, Volume: 20, Issue:20 | Structure-activity relationship study of nitrosopyrimidines acting as antifungal agents. |
| AID1171989 | Antibacterial activity against Shigella flexneri MTCC 1457 assessed as inhibition of visual growth after 24 hrs | 2015 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2 | Facile and diastereoselective synthesis of 3,2'-spiropyrrolidine-oxindoles derivatives, their molecular docking and antiproliferative activities. |
| AID270826 | Inhibition of rat testis 17-alpha-hydroxylase component of P450-17alpha at 10 uM | 2006 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 16, Issue:18 | Synthesis, biochemical evaluation and rationalisation of the inhibitory activity of a range of 4-substituted phenyl alkyl imidazole-based inhibitors of the enzyme complex 17alpha-hydroxylase/17,20-lyase (P450(17alpha)). |
| AID425716 | Antimicrobial activity against Balamuthia mandrillaris ATCC 50209 infected in HBMEC assessed as inhibition of encystment at 5 ug/mL after 7 days | 2007 | Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12 | Effect of antimicrobial compounds on Balamuthia mandrillaris encystment and human brain microvascular endothelial cell cytopathogenicity. |
| AID1557087 | Antifungal activity against Candida glabrata ATCC 66032 assessed as reduction in fungal cell growth incubated for 48 hrs by MTT based broth double dilution method | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Antifungal activity, mode of action variability, and subcellular distribution of coumarin-based antifungal azoles. |
| AID417961 | Antifungal activity against Saccharomyces cerevisiae after 48 hrs by broth microdilution technique | 2009 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6 | Relation between lipophilicity of alkyl gallates and antifungal activity against yeasts and filamentous fungi. |
| AID490996 | Antifungal activity against Aspergillus niger at 200 ug/disk after 48 hrs by disk diffusion method | 2010 | European journal of medicinal chemistry, Jul, Volume: 45, Issue:7 | Synthesis and bioassay of pyrrolyl oxazolines and thiazolines. |
| AID405108 | Antimicrobial activity against Mucor circinelloides assessed as percent of susceptible isolates after 24 hrs | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | In vitro susceptibilities of 217 clinical isolates of zygomycetes to conventional and new antifungal agents. |
| AID364764 | Inhibition of human recombinant CYP3A4 expressed in baculovirus-infected insect microsomes | 2008 | Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19 | Novel aldosterone synthase inhibitors with extended carbocyclic skeleton by a combined ligand-based and structure-based drug design approach. |
| AID262549 | Antifungal activity against Cryptococcus neoformans | 2006 | Journal of medicinal chemistry, Apr-20, Volume: 49, Issue:8 | Structure-based optimization of azole antifungal agents by CoMFA, CoMSIA, and molecular docking. |
| AID432802 | Antifungal activity against Sporothrix mexicana after 72 hrs by microdilution method | 2008 | Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2 | In vitro antifungal susceptibilities of five species of sporothrix. |
| AID1199392 | Inhibition of human CYP17 using 17alpha-hydroxypregnenolone substrate relative to control | 2015 | Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5 | Discovery and development of Galeterone (TOK-001 or VN/124-1) for the treatment of all stages of prostate cancer. |
| AID49634 | Minimum inhibitory concentration of compound for antifungal activity against Candida albicans 2 | 2000 | Bioorganic & medicinal chemistry letters, Oct-02, Volume: 10, Issue:19 | Novel antifungals based on 4-substituted imidazole: a combinatorial chemistry approach to lead discovery and optimization. |
| AID590696 | Antifungal activity against Aspergillus niger after 48 hrs by microdilution method | 2011 | European journal of medicinal chemistry, Apr, Volume: 46, Issue:4 | Synthesis and biological activity of 2-(bis((1,3,4-oxadiazolyl/1,3,4-thiadiazolyl)methylthio)methylene)malononitriles. |
| AID1129516 | Antimicrobial activity against Aspergillus niger after 24 hrs by broth dilution method | 2014 | European journal of medicinal chemistry, Apr-22, Volume: 77 | Synthesis, antimicrobial and cytotoxic activities of pyrimidinyl benzoxazole, benzothiazole and benzimidazole. |
| AID633914 | Antifungal activity against Candida albicans ATCC 90028 by twofold serial dilution technique | 2012 | European journal of medicinal chemistry, Jan, Volume: 47, Issue:1 | Isoxazoles incorporated N-substituted decahydroquinolines: a precursor to the next generation antimicrobial drug. |
| AID340018 | Cytotoxicity against human Caco-2 cells assessed as viability upto 100 uM by MTT assay | 2008 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14 | Synthesis of novel ketoconazole derivatives as inhibitors of the human Pregnane X Receptor (PXR; NR1I2; also termed SXR, PAR). |
| AID681122 | TP_TRANSPORTER: inhibition of Calcein-AM efflux in MDR1-expressing LLC-PK1 cells | 2003 | Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9 | Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery. |
| AID340962 | Antifungal activity against sCandida stellata isolates from grapes by NCCLS M27-A2 method | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8 | Cross-resistance to medical and agricultural azole drugs in yeasts from the oropharynx of human immunodeficiency virus patients and from environmental Bavarian vine grapes. |
| AID1174185 | Inhibition of human CYP17 expressed in Escherichia coli using [3H]-progesterone substrate pre-incubated for 5 mins in presence of rat P450 reductase by HPLC method | 2015 | European journal of medicinal chemistry, Jan-07, Volume: 89 | Discovery of new 7-substituted-4-imidazolylmethyl coumarins and 4'-substituted-2-imidazolyl acetophenones open analogues as potent and selective inhibitors of steroid-11β-hydroxylase. |
| AID566954 | Antifungal activity against Cryptococcus neoformans ATCC 32264 assessed as inhibition of fungal growth at 100 uM after 48 hrs by microplate analysis | 2011 | European journal of medicinal chemistry, Jan, Volume: 46, Issue:1 | Penetratin analogues acting as antifungal agents. |
| AID69488 | Minimum inhibitory concentration against Escherichia coli ATCC 25853 by agar plate dilution method; NT=Not tested | 2004 | Bioorganic & medicinal chemistry letters, Feb-09, Volume: 14, Issue:3 | Synthesis and antifungal activities of phenylenedithioureas. |
| AID319755 | Antimicrobial activity against Trichophyton rubrum isolates | 2008 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 18, Issue:11 | Synthesis and SAR studies of biaryloxy-substituted triazoles as antifungal agents. |
| AID1075569 | Antimicrobial activity against Candida albicans ATCC 22019 after 18 to 24 hrs by microbroth dilution method | 2014 | European journal of medicinal chemistry, Mar-03, Volume: 74 | Synthesis and biological evaluation of thiazoline derivatives as new antimicrobial and anticancer agents. |
| AID428319 | Inhibition of P-gp in human Caco-2 cells assessed as decrease in efflux permeability from basolateral to apical side at 50 uM after 120 mins | 2009 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15 | Synthesis and antimultidrug resistance evaluation of icariin and its derivatives. |
| AID592052 | Inhibition of human CYP3A4 expressed in baculovirus-infected insect microsomes | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7 | Fine-tuning the selectivity of aldosterone synthase inhibitors: structure-activity and structure-selectivity insights from studies of heteroaryl substituted 1,2,5,6-tetrahydropyrrolo[3,2,1-ij]quinolin-4-one derivatives. |
| AID207270 | Tested for inhibition of human testicular Steroid 17-alpha-hydroxylase/17,20 lyase | 1995 | Journal of medicinal chemistry, Oct-13, Volume: 38, Issue:21 | Esters of 3-pyridylacetic acid that combine potent inhibition of 17 alpha-hydroxylase/C17,20-lyase (cytochrome P45017 alpha) with resistance to esterase hydrolysis. |
| AID362813 | Antifungal activity against Aspergillus niger at 200 ug after 48 hrs by agar disc-diffusion method | 2008 | European journal of medicinal chemistry, May, Volume: 43, Issue:5 | Synthesis and antimicrobial activity of novel sulfone-linked bis heterocycles. |
| AID1456581 | Antifungal activity against Aspergillus fumigatus isolate 7544 by micro-broth dilution method | 2017 | Bioorganic & medicinal chemistry letters, 05-15, Volume: 27, Issue:10 | Design, synthesis, and in vitro evaluation of novel antifungal triazoles. |
| AID486234 | Antifungal activity against Candida albicans ATCC 10231 after 48 hrs | 2010 | European journal of medicinal chemistry, Jun, Volume: 45, Issue:6 | Naftifine-analogues as anti-Trypanosoma cruzi agents. |
| AID574062 | Antifungal activity against 10'5 cells/ml wild-type Candida albicans BF-1 by EUCAST method | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | Cell density and cell aging as factors modulating antifungal resistance of Candida albicans biofilms. |
| AID73609 | The compound was evaluated for mean zone diameter (inhibition) against filamentous fungi at 250 ug/mL concentration | 1987 | Journal of medicinal chemistry, Aug, Volume: 30, Issue:8 | Lysosomotropic agents. 7. Broad-spectrum antifungal activity of lysosomotropic detergents. |
| AID364066 | Antifungal activity against Candida albicans ATCC 10231 after 48 hrs by MTT assay | 2008 | European journal of medicinal chemistry, Sep, Volume: 43, Issue:9 | Enamines as novel antibacterials and their structure-activity relationships. |
| AID1301003 | Inhibition of human recombinant CYP1A2 using CEC as substrate incubated for 30 mins by fluorimetry | 2016 | European journal of medicinal chemistry, Jul-19, Volume: 117 | 2-hydroxyisoquinoline-1,3(2H,4H)-diones (HIDs) as human immunodeficiency virus type 1 integrase inhibitors: Influence of the alkylcarboxamide substitution of position 4. |
| AID340956 | Antifungal activity against Candida krusei ATCC 6258 by NCCLS M27-A2 method | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8 | Cross-resistance to medical and agricultural azole drugs in yeasts from the oropharynx of human immunodeficiency virus patients and from environmental Bavarian vine grapes. |
| AID340020 | Cytotoxicity against human SKOV3 cells assessed as viability upto 100 uM by MTT assay | 2008 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14 | Synthesis of novel ketoconazole derivatives as inhibitors of the human Pregnane X Receptor (PXR; NR1I2; also termed SXR, PAR). |
| AID1075571 | Antimicrobial activity against Fusarium moniliforme NRRL 1866 after 48 to 72 hrs by microbroth dilution method | 2014 | European journal of medicinal chemistry, Mar-03, Volume: 74 | Synthesis and biological evaluation of thiazoline derivatives as new antimicrobial and anticancer agents. |
| AID48601 | The compound was tested for antifungal activity against Candida stellatoidea MY1017 using agar dilution assay | 1987 | Journal of medicinal chemistry, Aug, Volume: 30, Issue:8 | Lysosomotropic agents. 7. Broad-spectrum antifungal activity of lysosomotropic detergents. |
| AID285159 | Antimicrobial activity against non replicating persistence Mycobacterium tuberculosis H37Rv in aerobic condition assessed by relative light units after 7 days | 2007 | Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4 | Low-oxygen-recovery assay for high-throughput screening of compounds against nonreplicating Mycobacterium tuberculosis. |
| AID48057 | The compound was tested for antifungal activity against Candida parapsilosis MY1009 using agar dilution assay | 1987 | Journal of medicinal chemistry, Aug, Volume: 30, Issue:8 | Lysosomotropic agents. 7. Broad-spectrum antifungal activity of lysosomotropic detergents. |
| AID1300880 | Antifungal activity against Candida tropicalis clinical isolate after 24 hrs by broth microdilution method | 2016 | European journal of medicinal chemistry, Jul-19, Volume: 117 | Novel 1,3-thiazolidin-4-one derivatives as promising anti-Candida agents endowed with anti-oxidant and chelating properties. |
| AID1221961 | Apparent permeability from basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY335979 | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2 | Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
| AID659900 | Antifungal activity against Saccharomyces cerevisiae at 50 ug/ml after 24 hrs by agar well diffusion assay | 2012 | European journal of medicinal chemistry, Jun, Volume: 52 | Design and synthesis of new 4-pyrazolin-3-yl-1,2,3-triazoles and 1,2,3-triazol-4-yl-pyrazolin-1-ylthiazoles as potential antimicrobial agents. |
| AID394835 | Inhibition of human sterol 14-alpha-demethylase assessed as drug/enzyme molar ratio required to produce 50 percent decrease in turnover number | 2009 | Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6 | Rational modification of a candidate cancer drug for use against Chagas disease. |
| AID48260 | Percent resistance against all Candida. species (40 clinical isolates) at 256 micro g/mL (pH=7.2), activity is expressed as R%. | 1995 | Journal of medicinal chemistry, Oct-13, Volume: 38, Issue:21 | Antifungal agents. 9. 3-Aryl-4-[alpha-(1H-imidazol-1-yl)arylmethyl]pyrroles: a new class of potent anti-Candida agents. |
| AID404141 | Antifungal activity against Aspergillus fumigatus 04-486 | 2005 | Journal of natural products, Nov, Volume: 68, Issue:11 | Extraction, hemisynthesis, and synthesis of canthin-6-one analogues. Evaluation of their antifungal activities. |
| AID1328088 | Antibacterial activity against Staphylococcus aureus after 24 hrs by broth dilution method | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | Synthesis and antimicrobial activity of styryl/pyrrolyl/pyrazolyl sulfonylmethyl-1,3,4-oxadiazolyl amines and styryl/pyrrolyl/pyrazolyl sulfonylmethyl-1,3,4-thiadiazolyl amines. |
| AID45494 | In vitro evaluation of minimum inhibitory concentration against Candida albicans 76 | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20 | Synthesis and antifungal activity of new azole derivatives containing an N-acylmorpholine ring. |
| AID284092 | Antifungal activity against Candida glabrata C115-2000 after 48 hrs | 2007 | Bioorganic & medicinal chemistry, Jan-01, Volume: 15, Issue:1 | Synthesis and antifungal activity of (Z)-5-arylidenerhodanines. |
| AID340953 | Antifungal activity against Candida glabrata isolates from feeding stuffs by NCCLS M27-A2 method | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8 | Cross-resistance to medical and agricultural azole drugs in yeasts from the oropharynx of human immunodeficiency virus patients and from environmental Bavarian vine grapes. |
| AID99365 | Binding constant for L244A mutant cytochrome P450cam expressed in Escherichia coli | 2004 | Journal of medicinal chemistry, Jul-01, Volume: 47, Issue:14 | Computer-assisted design of selective imidazole inhibitors for cytochrome p450 enzymes. |
| AID340960 | Antifungal activity against Candida rugosa isolates from feeding stuff by NCCLS M27-A2 method | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8 | Cross-resistance to medical and agricultural azole drugs in yeasts from the oropharynx of human immunodeficiency virus patients and from environmental Bavarian vine grapes. |
| AID282480 | Inhibition of human CYP24 hydroxylase expressed in V79 cells | 2004 | Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27 | Potent, selective and low-calcemic inhibitors of CYP24 hydroxylase: 24-sulfoximine analogues of the hormone 1alpha,25-dihydroxyvitamin D(3). |
| AID363713 | Antifungal activity against Aspergillus fumigatus ATTC 26934 after 48 hrs by broth microdilution technique | 2008 | Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17 | In vitro antifungal activity of polyfunctionalized 2-(hetero)arylquinolines prepared through imino Diels-Alder reactions. |
| AID284088 | Antifungal activity against Candida albicans C127-2000 after 48 hrs | 2007 | Bioorganic & medicinal chemistry, Jan-01, Volume: 15, Issue:1 | Synthesis and antifungal activity of (Z)-5-arylidenerhodanines. |
| AID574254 | Antifungal activity against 48 hrs cultures of 10'7 cells/ml Candida albicans ATCC 90028 biofilms by XTT reduction assay | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | Cell density and cell aging as factors modulating antifungal resistance of Candida albicans biofilms. |
| AID555814 | Antifungal activity against azole-susceptible Candida albicans 5457 after 48 hrs | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | Relative contributions of the Candida albicans ABC transporters Cdr1p and Cdr2p to clinical azole resistance. |
| AID311903 | Growth inhibition of Cladosporium herbarum at 0.25 mg after 72 hrs | 2007 | Journal of natural products, Dec, Volume: 70, Issue:12 | Bioactive polychlorinated bibenzyls from the liverwort Riccardia polyclada. |
| AID1068782 | Antifungal activity against Aspergillus niger at 100 ug/well after 48 hrs by agar well diffusion method | 2014 | European journal of medicinal chemistry, Feb-12, Volume: 73 | Synthesis and antimicrobial activity of (1,4-phenylene)bis(arylsulfonylpyrazoles and isoxazoles). |
| AID488640 | Antimicrobial activity against Candida tropicalis CT by broth dilution method | 2010 | Journal of natural products, Jun-25, Volume: 73, Issue:6 | Alkaloids from the bark of Guatteria hispida and their evaluation as antioxidant and antimicrobial agents. |
| AID594130 | Antimicrobial activity against Bacillus subtilis ATCC 6633 after 24 hrs by agar well diffusion method | 2011 | European journal of medicinal chemistry, May, Volume: 46, Issue:5 | Synthesis, antimicrobial, antioxidant, anti-hemolytic and cytotoxic evaluation of new imidazole-based heterocycles. |
| AID396954 | Antifungal activity against Curvularia lunata NCIM 716 at 100 ug/disk after 48 hrs by agar disc-diffusion method | 2009 | European journal of medicinal chemistry, May, Volume: 44, Issue:5 | Synthesis, antimicrobial and cytotoxic activities of 1,3,4-oxadiazoles, 1,3,4-thiadiazoles and 1,2,4-triazoles. |
| AID491002 | Antifungal activity against Curvularia lunata after 48 hrs by microdilution susceptibility assay | 2010 | European journal of medicinal chemistry, Jul, Volume: 45, Issue:7 | Synthesis and bioassay of pyrrolyl oxazolines and thiazolines. |
| AID37848 | Inhibition of Aspergillus fumigatus 231 growth for 48 hours in vitro. | 2001 | Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17 | 3-Phenyl-5-acyloxymethyl-2H,5H-furan-2-ones: synthesis and biological activity of a novel group of potential antifungal drugs. |
| AID633956 | Antifungal activity against Trichoderma viride IAM 5061 after 72 hrs by serial dilution technique | 2011 | Bioorganic & medicinal chemistry, Dec-15, Volume: 19, Issue:24 | Novel (E)-1-(4-methyl-2-(alkylamino)thiazol-5-yl)-3-arylprop-2-en-1-ones as potent antimicrobial agents. |
| AID405109 | Antimicrobial activity against Rhizomucor sp. assessed as percent of susceptible isolates after 24 hrs | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | In vitro susceptibilities of 217 clinical isolates of zygomycetes to conventional and new antifungal agents. |
| AID733706 | Antifungal activity against Malassezia pachydermatis at 1 mg/disc after 48 hrs by disc diffusion method | 2013 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6 | Facile one-pot synthesis of novel dispirooxindole-pyrrolidine derivatives and their antimicrobial and anticancer activity against A549 human lung adenocarcinoma cancer cell line. |
| AID1061737 | Antimicrobial activity against Aspergillus fumigatus by broth microdilution method | 2014 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1 | Synthesis and evaluation of novel azoles as potent antifungal agents. |
| AID179679 | Tested for efficacy of compound in experimental vaginal candidosis (rat) after tropical treatment at dosage of 9x 0.1% drug concentration | 1994 | Journal of medicinal chemistry, Jun-24, Volume: 37, Issue:13 | Derivatives of a novel cyclopeptolide. 1. Synthesis, antifungal activity, and structure-activity relationships. |
| AID1079937 | Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source] | |||
| AID405070 | Antifungal activity against Candida parapsilosis ATCC 22019 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by Sensititre YeastOne method | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods. |
| AID1110737 | Antifungal activity against Trichophyton mentagrophytes 445 after 120 hr by microdilution broth method | 2002 | Farmaco (Societa chimica italiana : 1989), Feb, Volume: 57, Issue:2 | Ring substituted 3-phenyl-1-(2-pyrazinyl)-2-propen-1-ones as potential photosynthesis-inhibiting, antifungal and antimycobacterial agents. |
| AID340957 | Antifungal activity against Candida lambica isolates from grapes by NCCLS M27-A2 method | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8 | Cross-resistance to medical and agricultural azole drugs in yeasts from the oropharynx of human immunodeficiency virus patients and from environmental Bavarian vine grapes. |
| AID53239 | Binding affinity for Cytochrome P450 17A1 (17-alpha-hydroxypregnenolone Km=560 nM) | 1998 | Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6 | Novel 17-azolyl steroids, potent inhibitors of human cytochrome 17 alpha-hydroxylase-C17,20-lyase (P450(17) alpha): potential agents for the treatment of prostate cancer. |
| AID1307853 | Inhibition of CYP3A4 in human liver microsomes using testosterone as substrate after 5 mins by LC-MS analysis | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7 | Understanding Oxadiazolothiazinone Biological Properties: Negative Inotropic Activity versus Cytochrome P450-Mediated Metabolism. |
| AID566948 | Antifungal activity against Candida albicans ATCC 10231 assessed as inhibition of fungal growth at 100 uM after 24 hrs by microplate analysis | 2011 | European journal of medicinal chemistry, Jan, Volume: 46, Issue:1 | Penetratin analogues acting as antifungal agents. |
| AID1328081 | Antifungal activity against Aspergillus niger assessed as inhibition of spore germination at 100 ug/well after 48 hrs by agar well diffusion method | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | Synthesis and antimicrobial activity of styryl/pyrrolyl/pyrazolyl sulfonylmethyl-1,3,4-oxadiazolyl amines and styryl/pyrrolyl/pyrazolyl sulfonylmethyl-1,3,4-thiadiazolyl amines. |
| AID49094 | The compound was tested for antifungal activity against Candida albicans MY1055 using agar dilution assay | 1987 | Journal of medicinal chemistry, Aug, Volume: 30, Issue:8 | Lysosomotropic agents. 7. Broad-spectrum antifungal activity of lysosomotropic detergents. |
| AID486239 | Antifungal activity against Aspergillus flavus ATCC 9170 after 48 hrs | 2010 | European journal of medicinal chemistry, Jun, Volume: 45, Issue:6 | Naftifine-analogues as anti-Trypanosoma cruzi agents. |
| AID415948 | Antimicrobial activity against Candida krusei by micro-broth dilution method | 2009 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6 | Design, synthesis, and biological evaluation of novel 1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluorophenyl)-3-substituted benzylamino-2-propanols. |
| AID406865 | Antimicrobial activity against Candida albicans GDH2346 dissociated biofilms at cell density of 10'8 cells/ml after 48 hrs by XTT assay | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | Role for cell density in antifungal drug resistance in Candida albicans biofilms. |
| AID1218829 | Inactivation of recombinant CYP3A4 (unknown origin) using midazolam as substrate assessed as recovery of enzyme activity at 1 uM preincubated for 5 mins followed by dialysis measured after 4 hrs | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7 | Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme. |
| AID1218830 | Inactivation of recombinant CYP3A4 (unknown origin) using testosterone as substrate assessed as recovery of enzyme activity at 1 uM preincubated for 5 mins followed by dialysis measured after 4 hrs | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7 | Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme. |
| AID117712 | Effect of oral administration (10 mg/kg) on recovery of Candida albicans from kidneys of mice with expt. candidal infection | 1983 | Journal of medicinal chemistry, Mar, Volume: 26, Issue:3 | Synthesis of (E)-1-(5-chlorothien-2-yl)-2-(1H-imidazol-1-yl)ethanone 2,6-dichlorophenylhydrazone hydrochloride, a novel, orally active antifungal agent. |
| AID262555 | Antifungal activity against Trichophyton violaceum | 2006 | Journal of medicinal chemistry, Apr-20, Volume: 49, Issue:8 | Structure-based optimization of azole antifungal agents by CoMFA, CoMSIA, and molecular docking. |
| AID131259 | Tested for efficacy of compound in experimental systemic candidosis (mouse) after oral treatment at dosage of 8 *100 mg kg e-1 | 1994 | Journal of medicinal chemistry, Jun-24, Volume: 37, Issue:13 | Derivatives of a novel cyclopeptolide. 1. Synthesis, antifungal activity, and structure-activity relationships. |
| AID551090 | Antifungal activity against Candida albicans at 1000 ug/mL after 72 hrs by agar diffusion assay | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1 | 3-[Benzimidazo- and 3-[benzothiadiazoleimidazo-(1,2-c)quinazolin-5-yl]-2H-chromene-2-ones as potent antimicrobial agents. |
| AID1103204 | Antifungal activity against Fusarium graminearum isolate CE171 after 48 to 72 hr | 2004 | Journal of agricultural and food chemistry, Jun-02, Volume: 52, Issue:11 | Antifungal chalcones and new caffeic acid esters from Zuccagnia punctata acting against soybean infecting fungi. |
| AID600776 | Fungicidal activity against Aspergillus fumigatus plant isolate after 72 hrs | 2011 | Bioorganic & medicinal chemistry, May-15, Volume: 19, Issue:10 | Thiazole-based chalcones as potent antimicrobial agents. Synthesis and biological evaluation. |
| AID530926 | Antifungal activity against Fluconazole resistant Candida albicans isolate 1 at 9.4 uM after 48 hrs by CLSI method | 2008 | Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7 | Potent in vitro antifungal activities of naturally occurring acetylenic acids. |
| AID486232 | Cytotoxicity against mouse J774 cells after 48 hrs by MTT assay | 2010 | European journal of medicinal chemistry, Jun, Volume: 45, Issue:6 | Naftifine-analogues as anti-Trypanosoma cruzi agents. |
| AID532569 | Antifungal activity against Candida glabrata isolate 21230 with silent mutation in ERG4, ERG5 genes and nonsense mutation in ERG6 gene by Etest method | 2008 | Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10 | A nonsense mutation in the ERG6 gene leads to reduced susceptibility to polyenes in a clinical isolate of Candida glabrata. |
| AID402396 | Antifungal activity against Saccharomyces cerevisiae 1353 | 1998 | Journal of natural products, Oct, Volume: 61, Issue:10 | DNA-damaging steroidal alkaloids from Eclipta alba from the suriname rainforest1. |
| AID687548 | Antifungal activity against Aspergillus niger ATCC 9029 by NCCLS broth microdilution method | 2012 | Bioorganic & medicinal chemistry, Oct-15, Volume: 20, Issue:20 | Structure-activity relationship study of nitrosopyrimidines acting as antifungal agents. |
| AID497819 | Antifungal activity against Fusarium sp. clinical isolates after 48 hrs by broth microdilution method | 2010 | Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1 | In vitro activity of thimerosal against ocular pathogenic fungi. |
| AID664300 | Antifungal activity against Aspergillus niger MTCC 282 at 100 ug/disc by paper disc diffusion technique | 2012 | European journal of medicinal chemistry, Jul, Volume: 53 | Synthesis of benzimidazolyl-1,3,4-oxadiazol-2ylthio-N-phenyl (benzothiazolyl) acetamides as antibacterial, antifungal and antituberculosis agents. |
| AID1160935 | Partition coefficient, log D of the compound at pH 7.4 | 2014 | Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21 | Orally bioavailable 6-chloro-7-methoxy-4(1H)-quinolones efficacious against multiple stages of Plasmodium. |
| AID1209490 | Antagonist activity at human PXR expressed in human HepG2 cells coexpressing CYP3A4 assessed as inhibition of rifampicin-induced receptor activation at 30 uM after 24 hrs by dual luciferase reporter gene assay | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1 | Species-dependent and receptor-selective action of bilobalide on the function of constitutive androstane receptor and pregnane X receptor. |
| AID48949 | Tested for minimum inhibitory concentration against Candida albicans 90 (Candida albicans) at pH 6.5. | 1994 | Journal of medicinal chemistry, Jun-24, Volume: 37, Issue:13 | Derivatives of a novel cyclopeptolide. 1. Synthesis, antifungal activity, and structure-activity relationships. |
| AID1110739 | Antifungal activity against Candida glabrata 20/I after 48 hr by microdilution broth method | 2002 | Farmaco (Societa chimica italiana : 1989), Feb, Volume: 57, Issue:2 | Ring substituted 3-phenyl-1-(2-pyrazinyl)-2-propen-1-ones as potential photosynthesis-inhibiting, antifungal and antimycobacterial agents. |
| AID633958 | Antifungal activity against Aspergillus ochraceus ATCC 12066 incubated for 72 hrs followed by serial sub-cultivation for 72 hrs by serial dilution technique | 2011 | Bioorganic & medicinal chemistry, Dec-15, Volume: 19, Issue:24 | Novel (E)-1-(4-methyl-2-(alkylamino)thiazol-5-yl)-3-arylprop-2-en-1-ones as potent antimicrobial agents. |
| AID322164 | Antifungal activity against Candida kefyr C 123-2000 after 48 hrs by CLSI M27-A2 method | 2008 | Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1 | N-Phenyl and N-phenylalkyl-maleimides acting against Candida spp.: time-to-kill, stability, interaction with maleamic acids. |
| AID405046 | Antifungal activity against Sporothrix schenckii SSA29 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by Sensititre YeastOne method | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods. |
| AID1474167 | Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status | 2016 | Drug discovery today, Apr, Volume: 21, Issue:4 | DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans. |
| AID406863 | Antimicrobial activity against Candida albicans GDH2346 at planktonic cell density of 10'8 cells/ml after 48 hrs by XTT assay | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | Role for cell density in antifungal drug resistance in Candida albicans biofilms. |
| AID340951 | Antifungal activity against Candida albicans isolates from animals by NCCLS M27-A2 method | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8 | Cross-resistance to medical and agricultural azole drugs in yeasts from the oropharynx of human immunodeficiency virus patients and from environmental Bavarian vine grapes. |
| AID690956 | Antifungal activity against Candida albicans NCIM 3102 after 48 hrs by NCCLS agar well diffusion method | 2012 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20 | Synthesis, characterization and biological evaluation of some novel 2,4-thiazolidinediones as potential cytotoxic, antimicrobial and antihyperglycemic agents. |
| AID322158 | Antifungal activity against Candida albicans C 130-2000 after 48 hrs by CLSI M27-A2 method | 2008 | Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1 | N-Phenyl and N-phenylalkyl-maleimides acting against Candida spp.: time-to-kill, stability, interaction with maleamic acids. |
| AID1217575 | Half life in castrated pig plasma withdrawn from portal vein at 200 mg/kg dosed via intrajejunal route by UPLC-tandem mass spectrometry | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5 | In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole. |
| AID494005 | Antifungal activity against Cryptococcus neoformans ATCC 32264 assessed as inhibition of fungal growth at 50 uM | 2010 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 20, Issue:16 | New antifungal peptides. Synthesis, bioassays and initial structure prediction by CD spectroscopy. |
| AID530966 | Antifungal activity against Aspergillus fumigatus ATCC 204305 at 9.4 uM after 48 hrs by CLSI method | 2008 | Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7 | Potent in vitro antifungal activities of naturally occurring acetylenic acids. |
| AID1079948 | Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source] | |||
| AID405106 | Antimicrobial activity against Rhizopus microsporus var. microsporus assessed as percent of susceptible isolates after 24 hrs | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | In vitro susceptibilities of 217 clinical isolates of zygomycetes to conventional and new antifungal agents. |
| AID549785 | Inhibition of human CYP17 expressed in Escherichia coli using progesterone as substrate | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1 | N-(Pyridin-3-yl)benzamides as selective inhibitors of human aldosterone synthase (CYP11B2). |
| AID1308031 | Inhibition of CYP3A4 in human liver microsomes using midazolam as substrate at 10 uM preincubated for 5 mins followed by NADPH addition measured after 5 mins by LC-MS/MS analysis relative to control | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10 | Potent and Selective Human Neuronal Nitric Oxide Synthase Inhibition by Optimization of the 2-Aminopyridine-Based Scaffold with a Pyridine Linker. |
| AID456073 | Antifungal activity against Fulvia fulva TK 5318 after 72 hrs by serial sub-cultivation method | 2010 | Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1 | Novel 4-thiazolidinone derivatives as potential antifungal and antibacterial drugs. |
| AID420066 | Antifungal activity against Candida albicans PCA-2 after 24 hrs by broth microdilution assay | 2009 | Bioorganic & medicinal chemistry, Jun-01, Volume: 17, Issue:11 | Bulky 1,4-benzoxazine derivatives with antifungal activity. |
| AID575107 | Antifungal activity against Madurella mycetomatis isolate 39 by XTT assay | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Madurella mycetomatis is not susceptible to the echinocandin class of antifungal agents. |
| AID1238924 | Antifungal activity against Cryptococcus neoformans Cn18 (Serotype C) WTBF-106 by microbroth dilution method | 2015 | Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17 | Synthesis and antifungal evaluation of head-to-head and head-to-tail bisamidine compounds. |
| AID1216150 | Inhibition of human CYP4F2 in human liver microsomes assessed as fingolimod metabolism | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2 | CYP4F enzymes are responsible for the elimination of fingolimod (FTY720), a novel treatment of relapsing multiple sclerosis. |
| AID32669 | In vitro inhibition of Absidia corymbifera 272 growth for 24 hours. | 2001 | Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17 | 3-Phenyl-5-acyloxymethyl-2H,5H-furan-2-ones: synthesis and biological activity of a novel group of potential antifungal drugs. |
| AID494183 | Antimicrobial activity against Candida tropicalis by broth microdilution method | 2010 | European journal of medicinal chemistry, Aug, Volume: 45, Issue:8 | Antimicrobial activity and a SAR study of some novel benzimidazole derivatives bearing hydrazone moiety. |
| AID619211 | Antifungal activity against 10'5 CFU/mL Aspergillus niger MTCC 282 after 48 hrs by agar streak dilution method | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Synthesis and studies of novel 2-(4-cyano-3-trifluoromethylphenyl amino)-4-(quinoline-4-yloxy)-6-(piperazinyl/piperidinyl)-s-triazines as potential antimicrobial, antimycobacterial and anticancer agents. |
| AID491988 | Inhibition of CYP3A4 expressed in baculovirus infected insect microsomes | 2010 | Journal of medicinal chemistry, Jul-08, Volume: 53, Issue:13 | Isopropylidene substitution increases activity and selectivity of biphenylmethylene 4-pyridine type CYP17 inhibitors. |
| AID1265645 | Antifungal activity against Candida sake clinical isolate after 24 hrs by sabouraud dextrose broth based microdilution method | 2016 | European journal of medicinal chemistry, Jan-01, Volume: 107 | Anti-Candida activity and cytotoxicity of a large library of new N-substituted-1,3-thiazolidin-4-one derivatives. |
| AID284086 | Antifungal activity against Candida albicans C125-2000 after 48 hrs | 2007 | Bioorganic & medicinal chemistry, Jan-01, Volume: 15, Issue:1 | Synthesis and antifungal activity of (Z)-5-arylidenerhodanines. |
| AID1217572 | Cmax in castrated pig plasma withdrawn from femoral vein at 200 mg/kg dosed via intrajejunal route by UPLC-tandem mass spectrometry | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5 | In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole. |
| AID1196741 | Antifungal activity against Aspergillus parasiticus NRRL 465 after 72 hrs by broth microdilution assay | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | A novel series of thiazolyl-pyrazoline derivatives: synthesis and evaluation of antifungal activity, cytotoxicity and genotoxicity. |
| AID574257 | Antifungal activity against 10'8 cells/ml Candida albicans SC5314 planktonic cells by XTT reduction assay | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | Cell density and cell aging as factors modulating antifungal resistance of Candida albicans biofilms. |
| AID47581 | Evaluation of In vitro antifungal activity against Candida albicans 31 by broth macro dilution method | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20 | Synthesis and antifungal activity of new azole derivatives containing an N-acylmorpholine ring. |
| AID48263 | The compound was tested for percent resistance against all Candida. species (40 clinical isolates) at 256 micro g/mL (pH=5.8), activity is expressed as R%. | 1995 | Journal of medicinal chemistry, Oct-13, Volume: 38, Issue:21 | Antifungal agents. 9. 3-Aryl-4-[alpha-(1H-imidazol-1-yl)arylmethyl]pyrroles: a new class of potent anti-Candida agents. |
| AID48270 | Tested In vitro for antifungal activity against candida Spp (Candida glabrata, Candida krusei) at pH 5.8 | 2002 | Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13 | Antifungal agents. 10. New derivatives of 1-[(aryl)[4-aryl-1H-pyrrol-3-yl]methyl]-1H-imidazole, synthesis, anti-candida activity, and quantitative structure-analysis relationship studies. |
| AID405037 | Antifungal activity against Sporothrix schenckii P24255 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by Sensititre YeastOne method | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods. |
| AID362169 | Inhibition of recombinant CYP3A4 expressed in baculovirus-infected insect microsomes | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16 | Synthesis, biological evaluation, and molecular modeling of abiraterone analogues: novel CYP17 inhibitors for the treatment of prostate cancer. |
| AID456837 | Antifungal activity against Penicillium ochrochloron ATCC 9112 after 72 hrs by serial sub-cultivation method | 2010 | Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1 | Novel 4-thiazolidinone derivatives as potential antifungal and antibacterial drugs. |
| AID419388 | Antifungal activity against Aspergillus fumigatus ATCC 46645 at 100 ug/disk after 48 hrs by paper disk diffusion technique | 2009 | European journal of medicinal chemistry, May, Volume: 44, Issue:5 | Synthesis and anti-microbial screening of some Schiff bases of 3-amino-6,8-dibromo-2-phenylquinazolin-4(3H)-ones. |
| AID648383 | Antifungal activity against Botrytis cinerea after 48 to 72 hrs by twofold serial dilution method | 2012 | European journal of medicinal chemistry, May, Volume: 51 | Synthesis of novel spirooxindole derivatives by one pot multicomponent reaction and their antimicrobial activity. |
| AID1209455 | Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1 | In vitro inhibition of the bile salt export pump correlates with risk of cholestatic drug-induced liver injury in humans. |
| AID1451801 | Antifungal activity against Trichophyton mentagrophytes after 7 days | 2017 | Journal of medicinal chemistry, 10-12, Volume: 60, Issue:19 | Novel Inhibitors of Staphyloxanthin Virulence Factor in Comparison with Linezolid and Vancomycin versus Methicillin-Resistant, Linezolid-Resistant, and Vancomycin-Intermediate Staphylococcus aureus Infections in Vivo. |
| AID563608 | Effect on sterol composition in Candida albicans isolate 14 expressing wild type erg11 and erg5 assessed as ergosterol level after 2 hrs by gas chromatography | 2010 | Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9 | A clinical isolate of Candida albicans with mutations in ERG11 (encoding sterol 14alpha-demethylase) and ERG5 (encoding C22 desaturase) is cross resistant to azoles and amphotericin B. |
| AID325037 | Antimicrobial activity against Candida albicans SC5314 after 48 hrs by broth macrodilution method | 2007 | Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5 | A Candida albicans petite mutant strain with uncoupled oxidative phosphorylation overexpresses MDR1 and has diminished susceptibility to fluconazole and voriconazole. |
| AID575121 | Antifungal activity against Aspergillus fumigatus ATCC 204305 by XTT assay | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Madurella mycetomatis is not susceptible to the echinocandin class of antifungal agents. |
| AID1061740 | Antimicrobial activity against Cryptococcus neoformans after 72 hrs by broth microdilution method | 2014 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1 | Synthesis and evaluation of novel azoles as potent antifungal agents. |
| AID574263 | Antifungal activity against 24 hrs cultures of 10'7 cells/ml Candida albicans ATCC 90028 biofilms by XTT reduction method | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | Cell density and cell aging as factors modulating antifungal resistance of Candida albicans biofilms. |
| AID564271 | Antifungal activity against Candida albicans isolate 177 after 48 hrs by broth microdilution method | 2010 | Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9 | A clinical isolate of Candida albicans with mutations in ERG11 (encoding sterol 14alpha-demethylase) and ERG5 (encoding C22 desaturase) is cross resistant to azoles and amphotericin B. |
| AID340021 | Cytotoxicity against human CRL cells assessed as viability upto 100 uM by MTT assay | 2008 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14 | Synthesis of novel ketoconazole derivatives as inhibitors of the human Pregnane X Receptor (PXR; NR1I2; also termed SXR, PAR). |
| AID1473739 | Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1 | A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
| AID655583 | Antifungal activity against Candida parapsilosis by microbroth dilution method | 2012 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8 | New triazole derivatives as antifungal agents: synthesis via click reaction, in vitro evaluation and molecular docking studies. |
| AID313551 | Inhibition of hepatic CYP2C9 at 1 uM | 2008 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 18, Issue:1 | Synthesis, biological evaluation and molecular modelling studies of novel ACD- and ABD-ring steroidomimetics as inhibitors of CYP17. |
| AID1166507 | Cytotoxicity against Swiss mouse primary peritoneal macrophages assessed as growth inhibition at 50 uM after 48 hrs by SRB assay | 2014 | Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21 | Effect of dehydroepiandrosterone derivatives on the activity of 5α-reductase isoenzymes and on cancer cell line PC-3. |
| AID696540 | Antifungal activity against Aspergillus fumigatus ATCC 26934 after 48 hrs by broth microdilution technique | 2012 | Bioorganic & medicinal chemistry, Nov-01, Volume: 20, Issue:21 | Synthesis and antifungal activity of diverse C-2 pyridinyl and pyridinylvinyl substituted quinolines. |
| AID420667 | Antifungal activity against Aspergillus fumigatus by micro-broth dilution method | 2009 | European journal of medicinal chemistry, May, Volume: 44, Issue:5 | Design, synthesis, and biological evaluation of novel triazole derivatives as inhibitors of cytochrome P450 14alpha-demethylase. |
| AID362147 | Inhibition of human recombinant CYP17 expressed in Escherichia coli | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16 | Overcoming undesirable CYP1A2 inhibition of pyridylnaphthalene-type aldosterone synthase inhibitors: influence of heteroaryl derivatization on potency and selectivity. |
| AID396953 | Antifungal activity against Fusarium solani NCIM 1330 at 100 ug/disk after 48 hrs by agar disc-diffusion method | 2009 | European journal of medicinal chemistry, May, Volume: 44, Issue:5 | Synthesis, antimicrobial and cytotoxic activities of 1,3,4-oxadiazoles, 1,3,4-thiadiazoles and 1,2,4-triazoles. |
| AID774143 | Inhibition of CYP3A4 in human liver microsomes assessed as midazolam hydroxylation to 1'-hydroxymidazolam at 1 uM after 10 mins relative to control | 2013 | Journal of medicinal chemistry, Oct-10, Volume: 56, Issue:19 | Rational development of 4-aminopyridyl-based inhibitors targeting Trypanosoma cruzi CYP51 as anti-chagas agents. |
| AID532559 | Antifungal activity against Saccharomyces cerevisiae BY4741 assessed as growth rate at 2 ug/ml (Rvb = 0.144%) | 2008 | Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10 | Differential azole antifungal efficacies contrasted using a Saccharomyces cerevisiae strain humanized for sterol 14 alpha-demethylase at the homologous locus. |
| AID377679 | Antifungal activity against Pseudallescheria boydii after 48 hrs by NCCLS M27A method | 2006 | Journal of natural products, Jul, Volume: 69, Issue:7 | Phytochemistry and antifungal properties of the newly discovered tree Pleodendron costaricense. |
| AID1319261 | Inhibition of CYP3A4 in human liver microsomes using midazolam as substrate assessed as reduction in 1-OH-midazolam formation at 0.08 uM by LC/MS/MS analysis | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18 | Identification of (R)-(2-Chloro-3-(trifluoromethyl)phenyl)(1-(5-fluoropyridin-2-yl)-4-methyl-6,7-dihydro-1H-imidazo[4,5-c]pyridin-5(4H)-yl)methanone (JNJ 54166060), a Small Molecule Antagonist of the P2X7 receptor. |
| AID490993 | Antifungal activity against Curvularia lunata at 100 ug/disk after 48 hrs by disk diffusion method | 2010 | European journal of medicinal chemistry, Jul, Volume: 45, Issue:7 | Synthesis and bioassay of pyrrolyl oxazolines and thiazolines. |
| AID330529 | Antifungal activity against Candida parapsilosis infected cyclophosphamide-immunocompromized Crl:CD1(ICR) mouse assessed as fungal density in lung at 0.5 mg/kg, po for 5 days measured on day 12 | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Mar-13, Volume: 104, Issue:11 | High-throughput synergy screening identifies microbial metabolites as combination agents for the treatment of fungal infections. |
| AID515008 | Antifungal activity against Candida albicans SC5314 after 24 hrs by micro-broth dilution method | 2010 | European journal of medicinal chemistry, Oct, Volume: 45, Issue:10 | Synthesis and antifungal evaluation of novel triazole derivatives as inhibitors of cytochrome P450 14alpha-demethylase. |
| AID1157293 | Antifungal activity against Candida glabrata 537 assessed as growth inhibition by automatic microplate reader analysis | 2014 | Journal of natural products, May-23, Volume: 77, Issue:5 | Polyhydroxy cyclohexanols from a Dendrodochium sp. fungus associated with the sea cucumber Holothuria nobilis Selenka. |
| AID284098 | Antifungal activity against Candida tropicalis C131-1997 after 48 hrs | 2007 | Bioorganic & medicinal chemistry, Jan-01, Volume: 15, Issue:1 | Synthesis and antifungal activity of (Z)-5-arylidenerhodanines. |
| AID628510 | Antifungal activity against Aspergillus niger at 200 ug/ml after 48 hrs by disc diffusion method | 2011 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21 | Synthesis and biological evaluation of some novel triazol-3-ones as antimicrobial agents. |
| AID45326 | Evaluation of In vitro antifungal activity against Candida albicans 406 by broth macro dilution method | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20 | Synthesis and antifungal activity of new azole derivatives containing an N-acylmorpholine ring. |
| AID575105 | Antifungal activity against Madurella mycetomatis isolate 35 by XTT assay | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Madurella mycetomatis is not susceptible to the echinocandin class of antifungal agents. |
| AID1067048 | Antifungal activity against Candida albicans SC5314 after 24 hrs by micro-broth dilution method | 2014 | European journal of medicinal chemistry, Mar-03, Volume: 74 | Synthesis, antifungal activities and molecular docking studies of novel 2-(2,4-difluorophenyl)-2-hydroxy-3-(1H-1,2,4-triazol-1-yl)propyl dithiocarbamates. |
| AID555822 | Ratio of MIC50 for Candida albicans 5674 to MIC50 for cdr2/cdr2 deficient Candida albicans STY7 | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | Relative contributions of the Candida albicans ABC transporters Cdr1p and Cdr2p to clinical azole resistance. |
| AID1177652 | Selectivity ratio of IC50 for human CYP11B1 to IC50 for human CYP11B2 | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12 | Aldosterone synthase inhibitors as promising treatments for mineralocorticoid dependent cardiovascular and renal diseases. |
| AID566792 | Inhibition of human CYP3A4 | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2 | New drug-like hydroxyphenylnaphthol steroidomimetics as potent and selective 17β-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment of estrogen-dependent diseases. |
| AID47398 | In vitro antifungal activity against Candida albicans | 1984 | Journal of medicinal chemistry, Jul, Volume: 27, Issue:7 | Antimycotic azoles. 7. Synthesis and antifungal properties of a series of novel triazol-3-ones. |
| AID287719 | Ratio of IC50 for human THP1 cells to IC50 for Trypanosoma cruzi Y epimastigotes | 2007 | Bioorganic & medicinal chemistry, Apr-01, Volume: 15, Issue:7 | Second generation of 5-ethenylbenzofuroxan derivatives as inhibitors of Trypanosoma cruzi growth: synthesis, biological evaluation, and structure-activity relationships. |
| AID563614 | Effect on sterol composition in Candida albicans isolate 14 expressing wild type erg11 and erg5 assessed as lanosterol level after 2 hrs by gas chromatography | 2010 | Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9 | A clinical isolate of Candida albicans with mutations in ERG11 (encoding sterol 14alpha-demethylase) and ERG5 (encoding C22 desaturase) is cross resistant to azoles and amphotericin B. |
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| AID633992 | Antifungal activity against Saccharomyces cerevisiae ATCC 24657 assessed as growth inhibition at 31.2 uM after 24 to 48 hrs by agar plate bioassay | 2012 | European journal of medicinal chemistry, Jan, Volume: 47, Issue:1 | Antifungal activities of novel non-azole molecules against S. cerevisiae and C. albicans. |
| AID362810 | Antifungal activity against Curvularia lunata at 100 ug after 48 hrs by agar disc-diffusion method | 2008 | European journal of medicinal chemistry, May, Volume: 43, Issue:5 | Synthesis and antimicrobial activity of novel sulfone-linked bis heterocycles. |
| AID407009 | Antimicrobial activity against fluconazole-resistant Candida albicans FH5 at planktonic cell density of 10'8 cells/ml after 48 hrs by XTT assay | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | Role for cell density in antifungal drug resistance in Candida albicans biofilms. |
| AID477744 | Antimicrobial activity against Sporothrix schenckii after 24 hrs | 2010 | European journal of medicinal chemistry, Apr, Volume: 45, Issue:4 | An eco-friendly synthesis and antimicrobial activities of dihydro-2H-benzo- and naphtho-1,3-oxazine derivatives. |
| AID294852 | Antifungal activity against Aspergillus fumigatus after 7 days by micro-broth dilution method | 2007 | European journal of medicinal chemistry, Sep, Volume: 42, Issue:9 | Synthesis of novel triazole derivatives as inhibitors of cytochrome P450 14alpha-demethylase (CYP51). |
| AID49257 | Tested for minimum subinhibitory concentration against Candida albicans 88 (Candida albicans) at pH 6.5. | 1994 | Journal of medicinal chemistry, Jun-24, Volume: 37, Issue:13 | Derivatives of a novel cyclopeptolide. 1. Synthesis, antifungal activity, and structure-activity relationships. |
| AID1171986 | Antibacterial activity against Salmonella typhimurium MTCC 1251 assessed as inhibition of visual growth after 24 hrs | 2015 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2 | Facile and diastereoselective synthesis of 3,2'-spiropyrrolidine-oxindoles derivatives, their molecular docking and antiproliferative activities. |
| AID1252805 | Inhibition of human recombinant CYP3A4 assessed as conversion of luciferin-PPXE to D-luciferin at 10 uM by luminescence Glo assay relative to control | 2015 | European journal of medicinal chemistry, Oct-20, Volume: 103 | (2-Arylethenyl)-1,3,5-triazin-2-amines as a novel histamine H4 receptor ligands. |
| AID690957 | Antifungal activity against Aspergillus niger NCIM 548 after 48 hrs by NCCLS agar well diffusion method | 2012 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20 | Synthesis, characterization and biological evaluation of some novel 2,4-thiazolidinediones as potential cytotoxic, antimicrobial and antihyperglycemic agents. |
| AID1467470 | Antifungal activity against Fusarium oxysporum at 25 ug/ml after 48 hrs by agar well diffusion method | 2017 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 27, Issue:14 | Synthesis, SAR and molecular docking studies of benzo[d]thiazole-hydrazones as potential antibacterial and antifungal agents. |
| AID330527 | Antifungal activity against Candida parapsilosis infected cyclophosphamide-immunocompromized Crl:CD1(ICR) mouse assessed as fungal density in kidney at 10 mg/kg, po for 5 days measured on day 12 | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Mar-13, Volume: 104, Issue:11 | High-throughput synergy screening identifies microbial metabolites as combination agents for the treatment of fungal infections. |
| AID563615 | Effect on sterol composition in Candida albicans isolate 108 harboring erg11 and erg5 double mutant assessed as lanosterol level after 2 hrs by gas chromatography | 2010 | Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9 | A clinical isolate of Candida albicans with mutations in ERG11 (encoding sterol 14alpha-demethylase) and ERG5 (encoding C22 desaturase) is cross resistant to azoles and amphotericin B. |
| AID150736 | Fraction of high affinity at binding site of human P-Glycoprotein (P-gp) in two-affinity model | 2002 | Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26 | Pharmacophore model of drugs involved in P-glycoprotein multidrug resistance: explanation of structural variety (hypothesis). |
| AID300060 | Antifungal activity against Candida albicans at 50 ug after 48 hrs by disc diffusion method | 2007 | Bioorganic & medicinal chemistry, Aug-01, Volume: 15, Issue:15 | Synthesis, characterization and antimicrobial activity of new aliphatic sulfonamide. |
| AID452383 | Inhibition of Yarrowia lipolytica 24-SMT assessed as lanosterol-3-trimethylsilyl derivative at 0.2 ug/mL after 48 hrs by GC-MS analysis relative to untreated control | 2009 | Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23 | Side chain azasteroids and thiasteroids as sterol methyltransferase inhibitors in ergosterol biosynthesis. |
| AID419356 | Antifungal activity against Curvularia lunata at 200 ug/disk after 48 hrs by agar disc-diffusion method | 2009 | European journal of medicinal chemistry, May, Volume: 44, Issue:5 | Synthesis and bioassay of a new class of heterocycles pyrrolyl oxadiazoles/thiadiazoles/triazoles. |
| AID1129517 | Antimicrobial activity against Penicillium chrysogenum after 24 hrs by broth dilution method | 2014 | European journal of medicinal chemistry, Apr-22, Volume: 77 | Synthesis, antimicrobial and cytotoxic activities of pyrimidinyl benzoxazole, benzothiazole and benzimidazole. |
| AID574061 | Antifungal activity against 10'5 cells/ml Candida albicans ATCC 90028 by EUCAST method | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | Cell density and cell aging as factors modulating antifungal resistance of Candida albicans biofilms. |
| AID1557077 | Antifungal activity against Candida albicans SN152 assessed as reduction in fungal cell growth incubated for 24 hrs by MTT based broth double dilution method | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Antifungal activity, mode of action variability, and subcellular distribution of coumarin-based antifungal azoles. |
| AID49464 | Antifungal activity in rat vaginal candidasis, 8 day postinfection with Candida. albicans SOB FM-391 | 1988 | Journal of medicinal chemistry, Oct, Volume: 31, Issue:10 | Studies on antifungal agents. 23. Novel substituted 3,5-diphenyl-3-(1H-imidazol-1-ylmethyl)- 2-alkylisoxazolidine derivatives. |
| AID1238921 | Antifungal activity against Candida krusei WTBF-51 by microbroth dilution method | 2015 | Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17 | Synthesis and antifungal evaluation of head-to-head and head-to-tail bisamidine compounds. |
| AID1217660 | AUC (0 to 6 hrs) in castrated pig plasma withdrawn from portal vein at 200 mg/kg dosed via intrajejunal route by UPLC-tandem mass spectrometry | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5 | In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole. |
| AID1324373 | Antifungal activity against Aspergillus niger by agar streak dilution method | 2016 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 26, Issue:22 | Novel substituted hydrazono indolo[2,1-b]quinazoline-6,12-dione analogues as cytostatic agents: Synthesis, crystal structure, biological evaluation and molecular docking studies. |
| AID1473741 | Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1 | A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
| AID456842 | Antifungal activity against Aspergillus niger ATCC 6275 after 72 hrs by serial dilution method | 2010 | Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1 | Novel 4-thiazolidinone derivatives as potential antifungal and antibacterial drugs. |
| AID54948 | Binding constant for wild type cytochrome P450cam expressed in Escherichia coli | 2004 | Journal of medicinal chemistry, Jul-01, Volume: 47, Issue:14 | Computer-assisted design of selective imidazole inhibitors for cytochrome p450 enzymes. |
| AID48806 | Minimum inhibitory concentration of compound for antifungal activity against Candida tropicalis | 2000 | Bioorganic & medicinal chemistry letters, Oct-02, Volume: 10, Issue:19 | Novel antifungals based on 4-substituted imidazole: a combinatorial chemistry approach to lead discovery and optimization. |
| AID449689 | Antifungal activity against Aspergillus niger NCIM 596 at 200 ug/disk after 48 hrs by agar disk diffusion method | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11 | Synthesis, antimicrobial and antioxidant activities of substituted pyrazoles, isoxazoles, pyrimidine and thioxopyrimidine derivatives. |
| AID405022 | Antifungal activity against Sporothrix schenckii P30019 isolate from cutaneous-lymphatic sporotrichosis patient after 72 hrs by Sensititre YeastOne method | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | In vitro susceptibility of Sporothrix schenckii to six antifungal agents determined using three different methods. |
| AID1304743 | Antifungal activity against Trichophyton verrucosum measured after 7 days by serial dilution method | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7 | Discovery of Potent Benzofuran-Derived Diapophytoene Desaturase (CrtN) Inhibitors with Enhanced Oral Bioavailability for the Treatment of Methicillin-Resistant Staphylococcus aureus (MRSA) Infections. |
| AID262551 | Antifungal activity against Fonsecaea pedrosoi | 2006 | Journal of medicinal chemistry, Apr-20, Volume: 49, Issue:8 | Structure-based optimization of azole antifungal agents by CoMFA, CoMSIA, and molecular docking. |
| AID420075 | Antifungal activity against Candida parapsilosis after 48 hrs by broth microdilution assay | 2009 | Bioorganic & medicinal chemistry, Jun-01, Volume: 17, Issue:11 | Bulky 1,4-benzoxazine derivatives with antifungal activity. |
| AID48072 | Evaluation of In vitro antifungal activity against Candida pseudotropicalis ATCC 28838 by broth macro dilution method | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20 | Synthesis and antifungal activity of new azole derivatives containing an N-acylmorpholine ring. |
| AID1265641 | Antifungal activity against Candida glabrata clinical isolate after 24 hrs by sabouraud dextrose broth based microdilution method | 2016 | European journal of medicinal chemistry, Jan-01, Volume: 107 | Anti-Candida activity and cytotoxicity of a large library of new N-substituted-1,3-thiazolidin-4-one derivatives. |
| AID1130381 | Antifungal activity against Sporothrix schenckii assessed as growth inhibition in sabouraud broth after 14 days | 1979 | Journal of medicinal chemistry, Aug, Volume: 22, Issue:8 | Antimycotic imidazoles. part 4. Synthesis and antifungal activity of ketoconazole, a new potent orally active broad-spectrum antifungal agent. |
| AID322162 | Antifungal activity against Candida coliculosa C 122-2000 after 48 hrs by CLSI M27-A2 method | 2008 | Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1 | N-Phenyl and N-phenylalkyl-maleimides acting against Candida spp.: time-to-kill, stability, interaction with maleamic acids. |
| AID42883 | Inhibition of Candida lusitaniae 2446/I growth for 48 hours in vitro. | 2001 | Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17 | 3-Phenyl-5-acyloxymethyl-2H,5H-furan-2-ones: synthesis and biological activity of a novel group of potential antifungal drugs. |
| AID1210017 | Inhibition of CYP2C9 in human liver microsomes using diclofenac as substrate after 8 mins by LC-MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5 | Identifying a selective substrate and inhibitor pair for the evaluation of CYP2J2 activity. |
| AID405095 | Antimicrobial activity against Rhizopus microsporus var. rhizopodiformis after 24 hrs | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | In vitro susceptibilities of 217 clinical isolates of zygomycetes to conventional and new antifungal agents. |
| AID549053 | Antifungal activity against Candida albicans CA138 after 48 hrs by broth microdilution method | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | In vitro activities of retigeric acid B alone and in combination with azole antifungal agents against Candida albicans. |
| AID48243 | The compound was tested for antifungal activity against Candida rugosa MY1022 using agar dilution assay | 1987 | Journal of medicinal chemistry, Aug, Volume: 30, Issue:8 | Lysosomotropic agents. 7. Broad-spectrum antifungal activity of lysosomotropic detergents. |
| AID54877 | Evaluation of In vitro antifungal activity against Cryptococcus neoformans 87 by broth macro dilution method | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20 | Synthesis and antifungal activity of new azole derivatives containing an N-acylmorpholine ring. |
| AID392156 | Inhibition of Cryptosporidium hominis TS-DHFR by spectroscopic assay | 2009 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2 | Novel non-active site inhibitor of Cryptosporidium hominis TS-DHFR identified by a virtual screen. |
| AID395655 | Antifungal activity against Cryptococcus neoformans ATCC 32264 assessed as growth inhibition at 12.5 uM after 48 hrs | 2009 | European journal of medicinal chemistry, Jan, Volume: 44, Issue:1 | Penetratin and derivatives acting as antifungal agents. |
| AID48249 | Inhibitory activity against Candida. species. (40 clinical isolates), determined at pH-5.8 | 1995 | Journal of medicinal chemistry, Oct-13, Volume: 38, Issue:21 | Antifungal agents. 9. 3-Aryl-4-[alpha-(1H-imidazol-1-yl)arylmethyl]pyrroles: a new class of potent anti-Candida agents. |
| AID214294 | Inhibition of Trichophyton mentagrophytes 445 growth for 120 hours in vitro. | 2001 | Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17 | 3-Phenyl-5-acyloxymethyl-2H,5H-furan-2-ones: synthesis and biological activity of a novel group of potential antifungal drugs. |
| AID1319264 | Inhibition of CYP3A4 in human liver microsomes using midazolam as substrate assessed as reduction in 4-OH-midazolam formation at 0.01 uM by LC/MS/MS analysis | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18 | Identification of (R)-(2-Chloro-3-(trifluoromethyl)phenyl)(1-(5-fluoropyridin-2-yl)-4-methyl-6,7-dihydro-1H-imidazo[4,5-c]pyridin-5(4H)-yl)methanone (JNJ 54166060), a Small Molecule Antagonist of the P2X7 receptor. |
| AID283205 | Antimicrobial activity against Candida glabrata 21231 isolate by E-test | 2007 | Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3 | Reduced susceptibility to polyenes associated with a missense mutation in the ERG6 gene in a clinical isolate of Candida glabrata with pseudohyphal growth. |
| AID1265644 | Antifungal activity against Candida parapsilosis clinical isolate after 24 hrs by sabouraud dextrose broth based microdilution method | 2016 | European journal of medicinal chemistry, Jan-01, Volume: 107 | Anti-Candida activity and cytotoxicity of a large library of new N-substituted-1,3-thiazolidin-4-one derivatives. |
| AID771363 | Growth inhibition of human PC3 cells at 50 uM after 48 hrs by SRB assay relative to control | 2013 | European journal of medicinal chemistry, Oct, Volume: 68 | Cytotoxic effect of novel dehydroepiandrosterone derivatives on different cancer cell lines. |
| AID530978 | Antifungal activity against Aspergillus flavus ATCC 204304 at 9.4 uM after 48 hrs by CLSI method | 2008 | Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7 | Potent in vitro antifungal activities of naturally occurring acetylenic acids. |
| AID429364 | Antifungal activity against Trichoderma viride at 1000 ug/ml after 72 hrs by agar diffusion method | 2009 | European journal of medicinal chemistry, Aug, Volume: 44, Issue:8 | Mono and bis-6-arylbenzimidazo[1,2-c]quinazolines: a new class of antimicrobial agents. |
| AID415952 | Antimicrobial activity against Candida tropicalis by micro-broth dilution method | 2009 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6 | Design, synthesis, and biological evaluation of novel 1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluorophenyl)-3-substituted benzylamino-2-propanols. |
| AID1224817 | Assays to identify small molecules inhibitory for eIF4E expression | 2015 | Chemistry & biology, Jul-23, Volume: 22, Issue:7 | Internal Ribosome Entry Site-Based Bicistronic In Situ Reporter Assays for Discovery of Transcription-Targeted Lead Compounds. |
| AID1346671 | Human Kv1.8 (Voltage-gated potassium channels) | 2000 | American journal of physiology. Renal physiology, Jun, Volume: 278, Issue:6 | KCNA10: a novel ion channel functionally related to both voltage-gated potassium and CNG cation channels. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 1540 (26.24) | 18.7374 |
| 1990's | 1490 (25.38) | 18.2507 |
| 2000's | 1287 (21.93) | 29.6817 |
| 2010's | 1263 (21.52) | 24.3611 |
| 2020's | 290 (4.94) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.
| This Compound (77.22) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Trials | 706 (11.38%) | 5.53% |
| Reviews | 16 (10.74%) | 6.00% |
| Reviews | 494 (7.97%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Case Studies | 1,113 (17.95%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Observational | 6 (0.10%) | 0.25% |
| Other | 133 (89.26%) | 84.16% |
| Other | 3,883 (62.61%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
| Trial | Phase | Enrollment | Study Type | Start Date | Status | ||
|---|---|---|---|---|---|---|---|
| Randomized Drug Interaction Study of RO4929097 for Advanced Solid Tumors [NCT01218620] | Phase 1 | 17 participants (Actual) | Interventional | 2010-09-30 | Completed | ||
| A Two-Way Interaction Study Between RO5190591/RTV and Ketoconazole in Healthy Subjects [NCT01164488] | Phase 1 | 18 participants (Actual) | Interventional | 2010-07-31 | Completed | ||
| A Phase 1, Open Label, Fixed-Sequence Study To Estimate The Effect Of Ketoconazole On The Pharmacokinetics Of Tasocitinib (CP-690,550) In Healthy Volunteers [NCT01202240] | Phase 1 | 12 participants (Actual) | Interventional | 2010-09-30 | Completed | ||
| A Phase I, Single Center, Open Label, 2-consecutive-group, 2-period, 1-sequence Crossover Study to Assess the Effect of Diltiazem (Cardizem), a Moderate CYP3A4 Inhibitor, or Ketoconazole, a Potent CYP3A4 Inhibitor, on the Pharmacokinetics of a Single Intr [NCT01124760] | Phase 1 | 28 participants (Actual) | Interventional | 2010-05-31 | Completed | ||
| Open Phase II Study of Ketoconazole as Inhibitor of the Enzyme CYP17 in Locally Advanced or Disseminated Granulosa Cell Tumour of Ovary. GreKo Study. [NCT01584297] | Phase 2 | 6 participants (Actual) | Interventional | 2012-10-31 | Terminated(stopped due to Insufficient recruitment rate) | ||
| Ph I Study to Assess the Effect of Ketoconazole on the Pharmacokinetics of Linifanib (ABT-869) [NCT01114191] | Phase 1 | 12 participants (Actual) | Interventional | 2010-05-31 | Completed | ||
| A Double-blind, Randomized, Placebo-controlled, Repeat Dose, 2-way Crossover Drug Interaction Study to Investigate the Pharmacokinetic and Pharmacodynamic Effects Following Administration of Fluticasone Furoate/GW642444M Inhalation Powder With Ketoconazol [NCT01165125] | Phase 1 | 18 participants (Actual) | Interventional | 2010-07-01 | Completed | ||
| Drug-Drug Interaction Study to Investigate the Effect of Ketoconazole on the Pharmacokinetic Properties of CKD-501 in Healthy Male Volunteer: Open, Randomised, 2-way Crossover, Clinical Trial [NCT01330563] | Phase 1 | 24 participants (Actual) | Interventional | 2011-03-31 | Completed | ||
| A Phase I, Non-Randomized, Open Label Study to Determine the Effetc of Ketoconazole on the Pharmacokinetics of a Single Oral Dose of Regorafenib (BAY73-4506) in Healthy Volunteers [NCT01318265] | Phase 1 | 24 participants (Actual) | Interventional | 2011-03-31 | Completed | ||
| Alterations in the Human Microbiome With Commonly Used Topical Medications [NCT03437005] | Phase 1 | 24 participants (Anticipated) | Interventional | 2013-01-28 | Recruiting | ||
| A Phase 2, Randomized, Vehicle and Ketoconazole-Controlled, Evaluator-Blinded, Study to Explore the Efficacy, Pharmacodynamics and Safety of Omiganan 1.75% Topical Gel BID in Patients With Mild to Moderate Facial Seborrheic Dermatitis [NCT03688971] | Phase 2 | 36 participants (Anticipated) | Interventional | 2018-10-22 | Recruiting | ||
| A Randomized, Open, Crossover Clinical Study to Investigate the Effects of Ketoconazole on the Pharmacokinetics of CG100649 in Healthy Male Volunteers [NCT01154764] | Phase 1 | 28 participants (Actual) | Interventional | 2009-10-31 | Completed | ||
| An Open-Label, Multicenter Study to Assess the Potential Effects of Ketoconazole on the Pharmacokinetics of Trabectedin in Subjects With Advanced Malignancies [NCT01267084] | Phase 1/Phase 2 | 12 participants (Actual) | Interventional | 2011-02-28 | Completed | ||
| A Phase 0 Clinical Trial of Two Candidate Azoles (Ketoconazole and Posaconazole) for Patients With Recurrent High Grade Glioma [NCT03763396] | Early Phase 1 | 30 participants (Anticipated) | Interventional | 2019-08-01 | Active, not recruiting | ||
| A 4 Week Randomized Double-blind Parallel Group Active Comparator Controlled Study of Elidel (Pimecrolimus) for the Treatment of Seborrheic Dermatitis [NCT00403559] | Phase 2 | 113 participants (Actual) | Interventional | 2007-05-07 | Completed | ||
| Phase 3, Multicenter, Double-blind, Randomized, Non-inferiority Clinical Trial of Dapaconazole Cream 2% (Biolab Sanus Farmacêutica Ltda.) Versus Ketoconazole Cream 2% (Nizoral®, Janssen-Cilag Farmacêutica Ltda.) in Patients With Tinea Pedis [NCT03320486] | Phase 3 | 360 participants (Actual) | Interventional | 2017-11-01 | Completed | ||
| Ketoconazole In Situ Gel Versus Terconazole Cream for Treatment of Vaginal Candidiasis [NCT03473418] | Phase 3 | 69 participants (Anticipated) | Interventional | 2018-04-01 | Not yet recruiting | ||
| The Study of Efficacy and Safety of 2% Ketoconazole Cream in Thai Females With Mild Degree of Post - Adolescence Acne [NCT03178994] | Phase 3 | 42 participants (Actual) | Interventional | 2017-08-01 | Completed | ||
| Risk of QT-prolongation and Torsade de Pointes in Patients Treated With Acute Medication in a University Hospital [NCT02068170] | 178 participants (Actual) | Observational | 2014-02-28 | Completed | |||
| Mechanisms of Hormonal Control of Spermatogenesis in Man [NCT02147964] | Phase 2 | 0 participants (Actual) | Interventional | 2019-06-30 | Withdrawn(stopped due to No funding was obtained for this study.) | ||
| An Open-Label, Proof of Concept Study to Determine the Safety and Efficacy of Ketoconazole 2% Foam in the Treatment of Pityrosporum Folliculitis [NCT00824863] | Phase 4 | 10 participants (Actual) | Interventional | 2008-12-31 | Completed | ||
| [NCT02198170] | Phase 1 | 18 participants (Actual) | Interventional | 2011-02-28 | Completed | ||
| A Four-Part, Open-Label Study to Evaluate the Effects of Repeat Dose GSK2118436 on the Single Dose Pharmacokinetics of Warfarin, the Effects of Repeat Dose Oral Ketoconazole and Oral Gemfibrozil on the Repeat Dose Pharmacokinetics of GSK2118436, and the R [NCT01340846] | Phase 1 | 48 participants (Actual) | Interventional | 2012-09-03 | Completed | ||
| A Prospective Randomized Phase III, Trial Comparing Consolidation Therapy With or Without Strontium-89 Following Induction Chemotherapy in Androgen-Independent Prostate Cancer [NCT00024167] | Phase 3 | 265 participants (Actual) | Interventional | 2002-04-30 | Terminated(stopped due to Terminated due to slow accrual) | ||
| A Phase 3b, Comparative and Randomized Study to Assess the Efficacy and Safety of an Intravaginal Ovule Combination of Ketoconazole and Clindamycin Compared With an Intravaginal Cream Combination of Tetracycline and Amphotericin B for the Treatment of Bac [NCT01293643] | Phase 3 | 99 participants (Actual) | Interventional | 2010-05-31 | Completed | ||
| A Phase II Study of Oral Calcitriol in Combination With Ketoconazole in Castration Resistant Prostate Cancer, Progressing Despite Primary ADT and Abiraterone [NCT03261336] | Phase 2 | 1 participants (Actual) | Interventional | 2017-01-06 | Terminated(stopped due to can not meet enrollment) | ||
| A PHASE 4, OPEN-LABEL STUDY TO ASSESS THE LONG-TERM SAFETY OF EXTINA (KETOCONAZOLE) FOAM, 2% IN THE TREATMENT OF SEBORRHEIC DERMATITIS [NCT00703846] | Phase 4 | 498 participants (Actual) | Interventional | 2008-06-30 | Completed | ||
| A Single Center, Randomized, Double-Blind, Crossover Study to Assess Buprenorphine Accumulation and Description of Its Metabolites During Co-Medication of BTDS and Ketoconazole, Used As a CYP3A4 Inhibitor, in Healthy Subjects [NCT01259115] | Phase 1 | 20 participants (Actual) | Interventional | 2002-10-31 | Completed | ||
| An Endocrinologically and Pharmacologically Directed Trial of Ketoconazole and Corticosteroids in Castration Resistant Prostate Cancer [NCT01036594] | Phase 2 | 32 participants (Actual) | Interventional | 2009-12-11 | Completed | ||
| An Open-Label, Phase I Study to Evaluate the Pharmacokinetics and Tolerance of Co-administration of Oral Multiple Dose of Ketoconazole and an IV (Bolus) Infusion of Eribulin in Patients With Advanced Solid Tumors [NCT01000376] | Phase 1 | 12 participants (Actual) | Interventional | 2009-02-28 | Completed | ||
| A Phase I/II Trial of Ketoconazole, Hydrocortisone, Dutasteride and Lapatinib (KHAD-L) in Castration Resistant Prostate Cancer With Pre- and Post-therapy Tumor Biopsies [NCT00953576] | Phase 1/Phase 2 | 11 participants (Actual) | Interventional | 2009-09-29 | Terminated(stopped due to The study terminated early due to concerns about drug toxicity.) | ||
| Effect of Ketoconazole Inhibition of CYP3A on Urinary Excretion of Docetaxel [NCT00697437] | Phase 2 | 10 participants (Actual) | Interventional | 2006-10-31 | Completed | ||
| Assessing PSA Response in Low Dose Ketoconazole in Hormone Refractory Prostate Cancer Patients Who Have Failed at Least One Prior Systemic Chemotherapy Regimen [NCT00895310] | Phase 2 | 30 participants (Actual) | Interventional | 2009-05-31 | Completed | ||
| Non-inferiority Phase II Trial Comparing BL123 (Biolab Sanus Farmacêutica Ltda.) Versus Ketoconazole (Nizoral® Janssen-Cilag) in Patients With Tinea Pedis [NCT02824926] | Phase 2 | 60 participants (Actual) | Interventional | 2014-07-31 | Completed | ||
| A Study of the Effect of Concomitant Administration of Ketoconazole or Fluconazole on the Pharmacokinetics of BMS-708163 in Healthy Subjects [NCT00860275] | Phase 1 | 30 participants (Actual) | Interventional | 2009-04-30 | Completed | ||
| A Double-blind, Placebo-controlled, Randomised, 2-way Crossover Drug Interaction Study to Investigate the Pharmacokinetic and Pharmacodynamic Effects Following Co-administration of GW642444M With Ketoconazole [NCT00866515] | Phase 1 | 20 participants (Actual) | Interventional | 2008-12-22 | Completed | ||
| Phase I Study of Fenretinide (4-HPR, NSC 374551) Lym-X-Sorb (LXS) Oral Powder Plus Ketoconazole Plus Vincristine in Patients With Recurrent or Resistant Neuroblastoma (IND #68,254) [NCT02163356] | Phase 1 | 4 participants (Actual) | Interventional | 2014-05-31 | Terminated(stopped due to drug supply) | ||
| Relative Bioavailability of Single Doses of 150 mg Dabigatran Etexilate (Capsule) When Administered Alone or in Combination With a Single Dose of 400 mg Ketoconazole (Tablet) or in Combination With 400 mg q.d. Ketoconazole (Tablet) at Steady State in Heal [NCT02170675] | Phase 1 | 24 participants (Actual) | Interventional | 2009-06-30 | Completed | ||
| Ascending Single Dose Study Of The Safety, Tolerability And Pharmacokinetics Of SAM-760 Administered Orally To Healthy Young And Healthy Elderly Subjects [NCT00948662] | Phase 1 | 124 participants (Actual) | Interventional | 2009-09-30 | Completed | ||
| An Open-label Study to Evaluate the Safety, Tolerability and Pharmacokinetics of Cytochrome P450 Probe Drugs in Healthy Adult Subjects [NCT00964106] | Phase 1 | 87 participants (Actual) | Interventional | 2009-08-26 | Completed | ||
| A Human Phase 0, Microdose Drug-Drug Interaction Study With [14C]-GSK706769 and Ketoconazole in Healthy Male Volunteers [NCT00975936] | Phase 1 | 12 participants (Actual) | Interventional | 2009-09-21 | Completed | ||
| A Phase III Randomized Trial for Evaluating Second Line Hormonal Therapy (Ketoconazole/Hydrocortisone) Versus Paclitaxel/Estramustine Combination Chemotherapy on Progression Free Survival in Asymptomatic Patients With a Rising PSA After Hormonal Therapy f [NCT00027859] | Phase 3 | 0 participants | Interventional | 2003-10-08 | Completed | ||
| A Phase 1 Randomized, Open-Label, Two-Period,Two-Sequence Crossover Study to Evaluate the Relative Oral Bioavailability of Levoketoconazole and Ketoconazole Tablets in Healthy Subjects [NCT04212000] | Phase 1 | 34 participants (Actual) | Interventional | 2019-12-16 | Completed | ||
| Investigation of Antipsoriatic Effects of UVB-induced Synthesis of 1alpha, 25-Dihydroxyvitamin D3 (1alpha, 25(OH)2D3, Calcitriol)in Keratinocytes of Psoriatic Skin, Using Cytochrom-P(CYP)Inhibitor Ketokonazol [NCT00678756] | Phase 2 | 12 participants (Anticipated) | Interventional | 2008-03-31 | Active, not recruiting | ||
| A Phase I, Open-Label, Three-Period, Fixed-Sequence Study To Estimate The Steady-State Effect Of Ketoconazole And Omeprazole On The Single-Dose Pharmacokinetics Of Dimebon [PF-01913539] In Healthy CYP2D6 EM And PM Subjects [NCT00931073] | Phase 1 | 24 participants (Anticipated) | Interventional | 2009-07-31 | Completed | ||
| Steady-State Feedback Actions of Testosterone on Luteinizing Hormone Secretion in Young and Older Men [NCT00431197] | Phase 1 | 40 participants (Anticipated) | Interventional | 2004-02-29 | Completed | ||
| A Phase Ib Study Administering Rapamycin (Sirolimus) With Ketoconazole in Patients With Advanced Malignancies [NCT00708591] | Phase 1 | 57 participants (Actual) | Interventional | 2004-10-31 | Completed | ||
| An Open-Label Drug-Drug Interaction Study to Assess the Effect of Ketoconazole on the Pharmacokinetics of JNJ-31001074 in Healthy Subjects [NCT00915746] | Phase 1 | 14 participants (Actual) | Interventional | 2009-11-30 | Completed | ||
| Rapid Hormonal Cycling as Treatment for Patients With Prostate Cancer: The Men's Cycle [NCT00586898] | Phase 2 | 36 participants (Actual) | Interventional | 2001-07-31 | Completed | ||
| An Open-Label Clinical Pharmacology Study of Brentuximab Vedotin (SGN-35) in Patients With CD30-Positive Hematologic Malignancies: CYP3A4 Drug-Drug Interactions, Excretion, and Special Populations [NCT01026415] | Phase 1 | 73 participants (Actual) | Interventional | 2009-12-31 | Completed | ||
| An Open, Randomised, Cross-over, Single Centre Pharmacokinetic (Phase I) Study of the Biliary Excretion Following Single Doses of AZD0837, Given in the Duodenum Via a Loc-I-Gut Catheter, Alone or in Combination With Ketoconazole (Once Daily for 4 Days), t [NCT00812344] | Phase 1 | 20 participants (Anticipated) | Interventional | 2008-12-31 | Completed | ||
| An Open-Label, 2-Part Study to Determine the Relative Bioavailability of a Tablet Formulation of GDC-0941 and the Effect of Ketoconazole on the Pharmacokinetics of the GDC-0941 Tablet [NCT01240226] | Phase 1 | 22 participants (Actual) | Interventional | 2010-11-30 | Completed | ||
| A Three Part Study in Healthy Adult Subjects to Evaluate the Safety, Tolerability and Pharmacokinetics of Repeat Escalating Oral Doses of GSK580416; the Safety, Tolerability, and Pharmacokinetics of GSK580416 Following a Loading Dose Regimen; and the Effe [NCT00680485] | Phase 1 | 96 participants | Interventional | 2007-06-30 | Terminated | ||
| An Open-label, Randomized, Two-period Crossover Study to Evaluate the Effect of Multiple Doses of Ketoconazole on the Pharmacokinetics of Darexaban and Metabolites in Young Healthy Male Subjects [NCT01405989] | Phase 1 | 26 participants (Actual) | Interventional | 2010-01-31 | Completed | ||
| Phase 3 Study, Randomized, Double-blind, Parallel to Evaluate Ketoconazole and Betamethasone Dipropionate(Candicort®) Compared to Clotrimazole and Dexamethasone Acetate(Baycuten N®) in Relief of Fungal Infections/Dermatophytosis Symptoms. [NCT02582177] | Phase 3 | 125 participants (Actual) | Interventional | 2019-06-11 | Completed | ||
| [NCT00768690] | Phase 1 | 45 participants (Actual) | Interventional | 2008-10-31 | Completed | ||
| [NCT00890318] | Phase 1 | 32 participants (Actual) | Interventional | 2009-04-30 | Completed | ||
| Efficacy and Safety of Clobetasol Propionate Shampoo 0.05% Used in Association With an Antifungal Shampoo in the Treatment of Moderate to Severe Scalp Seborrheic Dermatitis [NCT00862654] | Phase 3 | 326 participants (Actual) | Interventional | 2009-03-31 | Completed | ||
| A Randomized,Double-blind,Vehicle-controlled, Parallel-design,Multiple-site Study to Evaluate the Therapeutic Equivalence of Ketoconazole Cream 2% (Douglas Pharmaceuticals America Ltd) to Ketoconazole Cream 2% (Teva Pharmaceuticals USA Inc.) in the Treatm [NCT04203342] | Phase 3 | 682 participants (Actual) | Interventional | 2019-12-11 | Completed | ||
| A Phase I, Single-Centre, Open-Label, Randomized, One-sequence Crossover, Three-Group Study to Evaluate the Effect of Ketoconazole, Ritonavir and Erythromicin on the Safety and Pharmacokinetics of Avanafil (TA-1790) in Healthy Male Subjects [NCT00770042] | Phase 1 | 44 participants (Actual) | Interventional | 2008-10-31 | Completed | ||
| Acute Respiratory Distress Syndrome Clinical Network (ARDSNet) [NCT00000579] | Phase 3 | 0 participants | Interventional | 1994-09-30 | Completed | ||
| Neoadjuvant Therapy With Docetaxel and Ketoconazole in Patients With High-Risk Prostate Cancer: A Pilot Study [NCT00870714] | 20 participants (Anticipated) | Interventional | 2004-09-30 | Active, not recruiting | |||
| Đánh giá hiệu quả điều trị viêm da dầu ở đầu của dầu gội Thái Dương 3 và Thái Dương 7 (A Randomized, Double Blind, Placebo Controlled, Parallel Group, Phase 3 Trial to Evaluate the Safety and Efficacy Shampoos TD03 and TD07 in Scalp Diseases) [NCT03845348] | Phase 3 | 366 participants (Anticipated) | Interventional | 2019-05-22 | Recruiting | ||
| Phase III, Open Label, Randomized, Multicenter Study to Evaluate Efficacy, Tolerability & Safety of Combination of Clindamycin 100mg and Ketoconazole 400mg in Vaginal Capsules, Compared to Combination of Tetracycline 100mg and Amphotericin B 50mg in Vagin [NCT00889356] | Phase 3 | 160 participants (Anticipated) | Interventional | 2009-09-30 | Not yet recruiting | ||
| An Open-label, Three-treatment, Three-period, One-sequence, Crossover Study to Evaluate the Effect of Ketoconazole and Rifampicin on the Pharmacokinetics of Fimasartan in Healthy Male Volunteers [NCT00938262] | Phase 1 | 24 participants (Actual) | Interventional | 2009-04-30 | Completed | ||
| A Phase 1 Study to Assess the Effect of Ketoconazole on the Pharmacokinetics of ABT-263 (Navitoclax) [NCT01021358] | Phase 1 | 12 participants (Anticipated) | Interventional | 2010-01-31 | Completed | ||
| An Open-label, Randomized, Single Sequence, Two Period Study to Assess the Effect of Repeat Oral Dosing of Ketoconazole on the Pharmacokinetics of a Single Oral Dose of GSK962040 in Healthy Volunteers [NCT01039974] | Phase 1 | 6 participants (Actual) | Interventional | 2009-09-18 | Completed | ||
| Restoration of Muscle Following Hip Surgery [NCT00393848] | Phase 2 | 40 participants (Actual) | Interventional | 2006-10-31 | Completed | ||
| Ketoconazole Foam 2% for the Treatment of Versicolor [NCT00830388] | Phase 4 | 11 participants (Actual) | Interventional | 2008-11-30 | Completed | ||
| A Randomized, Double-Blind, Vehicle-Controlled, Parallel-Design, Multiple-Site Clinical Study to Evaluate the Therapeutic Equivalence of Ketoconazole Cream 2% (Encube Ethicals Pvt Ltd) to Ketoconazole Cream 2% (G&W Laboratories Inc.) in the Treatment of T [NCT03824912] | Phase 3 | 831 participants (Actual) | Interventional | 2018-08-23 | Completed | ||
| Phase II Trial to Assess the Activity of Ketoconazole Plus Lenalidomide in Patients With Prostate Cancer Progressive After Androgen Deprivation [NCT00460031] | Phase 2 | 34 participants (Actual) | Interventional | 2006-09-01 | Completed | ||
| A Phase 1, Open-Label Study to Assess the Effect of Ketoconazole on the Pharmacokinetics of NBI-98854 in Healthy Subjects [NCT01910480] | Phase 1 | 24 participants (Actual) | Interventional | 2013-07-31 | Completed | ||
| An Open Label Study to Investigate the Relative Bioavailability, Food Effect and Effect of Ketoconazole on the Rate and Extent of Absorption of Solid Dosage Formulation(s) of JNJ-40411813 [NCT01932320] | Phase 1 | 36 participants (Actual) | Interventional | 2010-02-28 | Completed | ||
| Open Label Study in Healthy Volunteers to Investigate the Effect of Ketoconazole 400mg on Pharmacokinetics of SB-773812 20mg [NCT00411866] | Phase 1 | 36 participants (Actual) | Interventional | 2006-10-13 | Completed | ||
| A Phase 1 Study to Assess the Effect of Ketoconazole on the Pharmacokinetics of ABT-199 [NCT01969669] | Phase 1 | 12 participants (Actual) | Interventional | 2013-12-31 | Completed | ||
| Effect of Ketoconazole on the Pharmacokinetics of Intravenous (IV) Vinflunine in Patients With Advanced Cancer [NCT00388557] | Phase 1 | 35 participants (Anticipated) | Interventional | 2005-10-31 | Completed | ||
| An Open-Label Drug-Drug Interaction Study to Assess the Effect of Ketoconazole on the Pharmacokinetics of Abiraterone (JNJ-589485) Following Administration of Abiraterone Acetate (JNJ-212082) Tablets in Healthy Male Subjects [NCT01588782] | Phase 1 | 20 participants (Actual) | Interventional | 2012-01-31 | Completed | ||
| A Phase I Open-label, 2-period Study to Evaluate the Influence of Multiple Oral Doses of Ketoconazole on the Single Dose Pharmacokinetics of Romidepsin in Subjects With Advanced Cancer [NCT01324310] | Phase 1 | 15 participants (Actual) | Interventional | 2011-04-01 | Completed | ||
| A Phase I/II Study of Oral Calcitriol in Combination With Ketoconazole in Androgen Independent Prostate Cancer [NCT00536991] | Phase 1/Phase 2 | 51 participants (Actual) | Interventional | 2006-10-31 | Terminated(stopped due to difficult to recruit) | ||
| Assessment of the Treatment of the Severely Burned With Anabolic Agents on Clinical Outcomes, Recovery and Rehabilitation [NCT00675714] | Phase 2/Phase 3 | 1,126 participants (Actual) | Interventional | 2004-01-31 | Terminated(stopped due to At the request of the study site, this study has been closed and access to study-related data is unavailable. We are unable to submit the results-data.) | ||
| A Double-Blind, Randomized, Parallel Group Comparison of Nizoral Cream (F012), Ketoconazole 2% Cream (F126) and Placebo (F000) in the Treatment of Interdigital Tinea Pedis [NCT01110330] | Phase 3 | 583 participants (Actual) | Interventional | 2007-07-31 | Terminated(stopped due to Unexpected discordant results between the KOH microscopy and mycological culture tests at three study sites in the UK.) | ||
| A Phase I, Single-centre, Randomised, Open, Three-way Crossover Study to Evaluate the Effect of Ketoconazole and Verapamil, Respectively, on the Pharmacokinetics of AZD1305 After Repeated Oral Adm of Ketoconazole and Verapamil and Single Oral Dosing of AZ [NCT00707551] | Phase 1 | 27 participants (Anticipated) | Interventional | 2008-07-31 | Completed | ||
| Non-inferiority, Phase III Clinical Trial Comparing Dapaconazole Cream 2% (Biolab Sanus Farmacêutica Ltda.) Versus Ketoconazole Cream 2% (Nizoral® Janssen-Cilag) in Patients With Tinea Pedis [NCT02606383] | Phase 3 | 0 participants (Actual) | Interventional | 2016-06-30 | Withdrawn | ||
| A Randomized, Open-Label, Drug-Drug Interaction Study To Evaluate The Effect Of Ketoconazole Or Rifampicin On The Pharmacokinetic Characteristics And Safety Of Lc15-0444 In Healthy Male Volunteers [NCT01426906] | Phase 1 | 24 participants (Actual) | Interventional | 2011-01-31 | Completed | ||
| tGLI1 as a Therapeutic Target in Brain Metastases: A Window of Opportunity Study in Breast Cancer Brain Metastases and Primary Gliomas [NCT03796273] | Early Phase 1 | 19 participants (Anticipated) | Interventional | 2019-03-13 | Recruiting | ||
| Phase II Trial to Assess the Activity of Ketoconazole and Mitoxantrone Plus GM-CSF in Patients With Progressive Hormone Refractory Prostate Cancer [NCT00447473] | Phase 2 | 31 participants (Actual) | Interventional | 2006-07-31 | Terminated(stopped due to PI decision) | ||
| A Phase 1, Randomized, Double-blind, Placebo-controlled Study Evaluating the Safety,Tolerability and Pharmacokinetics of Multiple Ascending Doses of JTK-853 Administered for Two Weeks in Healthy Subjects [NCT01473069] | Phase 1 | 41 participants (Actual) | Interventional | 2010-03-31 | Terminated | ||
| A Phase I, Randomized, Double-Blind Study to Assess the Effects of Repeat Oral Dosing of Ketoconazole on the Pharmacokinetics of Repeat Oral Dosing of Casopitant in Healthy Subjects [NCT00460707] | Phase 1 | 85 participants (Actual) | Interventional | 2007-04-16 | Completed | ||
| Cytochrome P450 Inhibition With Ketoconazole to Decrease Dosage and Costs of Dasatinib for Chronic Myelogenous Leukemia [NCT05638763] | Phase 2 | 15 participants (Anticipated) | Interventional | 2024-11-30 | Recruiting | ||
| A Two-Part Dose-Rising Study to Evaluate the Safety, Tolerability and Pharmacokinetics of SB-751689 When Administered as an Oral Formulation at Supratherapeutic Dose Levels in Healthy Adult Subjects. [NCT00468689] | Phase 1 | 15 participants (Actual) | Interventional | 2007-04-30 | Completed | ||
| A Phase 2b, Randomized, Double-Blind, Parallel-Group, Study of Safety and Efficacy of 16 Weeks of Treatment With DIO-902 or DIO-902 Placebo in Addition to Metformin and Atorvastatin or Atorvastatin Placebo in Subjects With Type 2 Diabetes Mellitus (Protoc [NCT00494663] | Phase 2 | 200 participants (Anticipated) | Interventional | 2007-07-31 | Terminated(stopped due to Program Terminated) | ||
| Effect of Oral Ketoconazole on the Pharmacokinetics of Oral Dexamethasone and Oral Hydrocortisone in Patients With Androgen Independent Prostate Cancer [NCT00559481] | 0 participants (Actual) | Interventional | 2007-10-31 | Withdrawn(stopped due to Withdrawn due to low accrual) | |||
| A Randomized Comparative Multicenter Trial of Fluconazole and Ketoconazole in the Treatment of Esophageal Candidiasis in Immunocompromised Patients [NCT00002304] | 0 participants | Interventional | Completed | ||||
| A PHASE III TWO-ARM RANDOMIZED STUDY COMPARING ANTIANDROGEN WITHDRAWAL ALONE VERSUS ANTIANDROGEN WITHDRAWAL COMBINED WITH KETOCONAZOLE AND HYDROCORTISON IN PATIENTS WITH ADVANCED PROSTAGE CANCER [NCT00002760] | Phase 3 | 260 participants (Actual) | Interventional | 1996-08-31 | Completed | ||
| A Randomized Phase II Trial of Taxol/VP-16/Estramustine vs. Ketoconazole/Doxorubicin/Vinblastine/Estramustine in Androgen Independent Prostate Cancer [NCT00003084] | Phase 2 | 75 participants (Actual) | Interventional | 1997-12-31 | Completed | ||
| An Open-Label, Fixed-Sequence, 2-Period Study to Determine the Effect of Ketoconazole on the Pharmacokinetics of GDC-0980 [NCT01473316] | Phase 1 | 22 participants (Actual) | Interventional | 2011-11-30 | Completed | ||
| A Phase 1, Open-Label, Two-Period, One-Sequence Crossover Study to Assess Pharmacokinetic Interaction of Multiple Dose Ketoconazole on Single Dose YM178 Oral Controlled Absorption System (OCAS) in Healthy Male and Female Adult Volunteers [NCT01476800] | Phase 1 | 24 participants (Actual) | Interventional | 2006-07-31 | Completed | ||
| A Phase I Study of Oral Calcitriol in Combination With Ketoconazole in Refractory Advanced Malignancies [NCT00238225] | Phase 1 | 15 participants (Actual) | Interventional | 2004-11-30 | Completed | ||
| A Phase 1/2a, Randomized, Placebo-Controlled, Double-Blind, Parallel-Group, Study of Safety, Tolerability, Pharmacokinetics and Activity of 14 Days of Oral Dosing With the 2S,4R Enantiomer of Ketoconazole (DIO-902) in Subjects With Type 2 Diabetes Mellitu [NCT00302224] | Phase 1/Phase 2 | 50 participants | Interventional | 2005-02-28 | Completed | ||
| A Randomized Phase 2 Trial of 177Lu Radiolabeled Monoclonal Antibody HuJ591 (177Lu-J591) and Ketoconazole in Patients With High-Risk Castrate Biochemically Relapsed Prostate Cancer After Local Therapy [NCT00859781] | Phase 2 | 55 participants (Actual) | Interventional | 2009-06-30 | Active, not recruiting | ||
| The Effect of Ketoconazole on the Pharmacokinetics and Pharmacodynamics of Ixabepilone In Patients With Advanced Cancer [NCT00096317] | Phase 1 | 29 participants (Actual) | Interventional | 2003-03-31 | Completed | ||
| A Randomized, Double-Blinded, Placebo-Controlled Study Observing the Efficacy of Selenium Sulfide 1% Shampoo, Ketoconazole 2% Shampoo, and Ciclopirox 1% Shampoo as Adjunctive Treatments for Tinea Capitis in Children [NCT00127868] | 47 participants (Actual) | Interventional | 2005-03-31 | Completed | |||
| An Open Label Study in Healthy Volunteers to Investigate the Effect of Ketoconazole on the Pharmacokinetics of GSK189075 [NCT00501397] | Phase 1 | 22 participants (Actual) | Interventional | 2007-02-28 | Completed | ||
| An Open-label, Two Period, Fixed Sequence Study of Healthy Subjects to Assess the Effect of Repeat Oral Dosing of Ketoconazole on the Pharmacokinetics of a Single Oral Dose of [GW679769] [NCT00404378] | Phase 1 | 15 participants (Actual) | Interventional | 2006-10-20 | Completed | ||
| An Open-label, 1-sequence, 3-period, 3-treatment, Crossover Study to Assess the Effects of Ketoconazole on the Pharmacokinetics of NKTR-118 in Healthy Subjects [NCT01520896] | Phase 1 | 22 participants (Actual) | Interventional | 2012-02-29 | Completed | ||
| Phase I/II Trial of Fenretinide/LXS Oral Powder (NSC 374551) Plus Ketoconazole in Recurrent Ovarian Cancer and Primary Peritoneal Carcinoma [NCT01535157] | Phase 1/Phase 2 | 12 participants (Actual) | Interventional | 2012-02-29 | Terminated(stopped due to drug combination not providing any efficacy. Will use this data in opening new trial) | ||
| "A Phase II Trial of Early Medical Adrenalectomy for D0.5 Prostate Cancer" [NCT00006371] | Phase 2 | 2 participants (Actual) | Interventional | 2000-05-31 | Terminated(stopped due to low accrual) | ||
| Phase II Trial Of Sequential Estramustine/Paclitaxel Followed By Doxorubicin/Ketoconazole In Patients With Androgen-Independent Prostate Cancer [NCT00014352] | Phase 2 | 0 participants | Interventional | 2000-09-30 | Completed | ||
| Feedback Control of FSH Secretion in the Human Male [NCT00392457] | 175 participants (Anticipated) | Interventional | 1995-07-31 | Completed | |||
| A Phase I, Pilot, Dose Finding Clinical Trial to Assess the Interaction Between Sunitinib and Ketoconazole to Reduce the Dose and Cost of Sunitinib for National Health System [NCT01548170] | Phase 1 | 12 participants (Actual) | Interventional | 2011-04-30 | Completed | ||
| Phase II Randomized Study of High-Dose Ketoconazole With or Without Alendronate Sodium in Patients With Androgen-Independent Metastastic Adenocarinoma of the Prostate [NCT00019695] | Phase 2 | 0 participants | Interventional | 1999-03-31 | Terminated | ||
| A Phase III Randomized Study of Patients With High Risk, Hormone-Naive Prostate Cancer: Androgen Blockade With 4 Cycles of Immediate Chemotherapy Versus Androgen Blockade With Delayed Chemotherapy [NCT00030654] | Phase 3 | 21 participants (Actual) | Interventional | 2002-10-31 | Completed | ||
| A Two Cohort, Open-label Study to Evaluate the Pharmacokinetics of GSK2847065, the Metabolite of Retosiban (GSK221149) After Single and Repeat Oral Doses, the Pharmacokinetics of GSK221149 Coadministered With a High Fat Meal, and the Pharmacokinetics of G [NCT01627587] | Phase 1 | 46 participants (Actual) | Interventional | 2011-12-12 | Completed | ||
| A Phase I Trial of High Dose Ketoconazole Plus Weekly Docetaxel in Metastatic Androgen Independent Prostate Cancer [NCT00032825] | Phase 1 | 674 participants (Actual) | Interventional | 2002-03-19 | Completed | ||
| A Pilot Study of The Treatment of Central Serous Chorioretinopathy With Ketoconazole. [NCT00211393] | Phase 2 | 5 participants (Actual) | Interventional | 2005-05-31 | Completed | ||
| Phase II Study of Docetaxel Combined With Ketoconazole in the First-line Treatment of Locally Advanced or Metastatic Breast Cancer Patients With Measurable Primary Breast Tumor [NCT00212095] | Phase 2 | 30 participants (Actual) | Interventional | 2005-06-30 | Completed | ||
| Phase I Study to Evaluate the Effect of Ketoconazole on the Pharmacokinetics of Dasatinib and the Effect of Dasatinib on Pharmacodynamic Markers in Patients With Advanced Solid Tumors [NCT00162214] | Phase 1 | 60 participants | Interventional | 2005-08-31 | Terminated | ||
| A Phase II Trial of Ketoconazole, Hydrocortisone and Dutasteride in Asymptomatic Hormone Refractory Prostate Cancer [NCT00673127] | Phase 2 | 57 participants (Actual) | Interventional | 2005-02-28 | Completed | ||
| Phase II Trial to Assess the Activity of Ketoconazole Plus GM-CSF in Patients With Prostate Cancer Progressive After Androgen Deprivation [NCT00309894] | Phase 2 | 49 participants (Actual) | Interventional | 2004-04-30 | Completed | ||
| Phase I Study of Fenretinide (4-HPR, NSC 374551) Lym-X-Sorb™ (LXS) Oral Powder in Patients With Recurrent or Resistant Neuroblastoma [NCT00295919] | Phase 1 | 80 participants (Actual) | Interventional | 2005-12-31 | Completed | ||
| A Single-Center, Open-Label, Parallel Study to Investigate the Effects of Multiple Doses of Ketoconazole on the Pharmacokinetics of a Single Oral Dose of RO4602522 in Healthy Male Subjects [NCT01625806] | Phase 1 | 34 participants (Actual) | Interventional | 2012-07-31 | Completed | ||
| An Open-Label, Sequential Design Study to Assess the Effect of Ketoconazole on the Pharmacokinetics of Ibrutinib in Healthy Subjects [NCT01626651] | Phase 1 | 21 participants (Actual) | Interventional | 2012-06-30 | Completed | ||
| An Open-label, Single-sequence Study in Two Cohorts of Healthy Subjects to Evaluate the Single-dose Pharmacokinetics of Tasimelteon Alone and in Combination With a CYP3A4 Inhibitor, Ketoconazole, or a CYP3A4 Inducer, Rifampin. [NCT01637636] | Phase 1 | 48 participants (Actual) | Interventional | 2012-06-30 | Completed | ||
| A Phase 1, Randomized, Open-Label, Two-Arm, Parallel Group Study of the Effect of Ketoconazole at Steady State on the Pharmacokinetics of a Single Dose of Isavuconazole in Healthy Adult Subjects [NCT01657838] | Phase 1 | 24 participants (Actual) | Interventional | 2012-05-31 | Completed | ||
| An Open-Label Study to Assess the Effects of Repeated Twice-Daily Doses of Ketoconazole on the Steady-State Pharmacokinetics of JNJ-38518168 in Healthy Subjects [NCT01690286] | Phase 1 | 33 participants (Actual) | Interventional | 2012-10-31 | Completed | ||
| Expanded Access Study of Fenretinide (4-HPR, NSC 374551) Lym-X-Sorb (LXS) Oral Powder Plus Ketoconazole in Patients With Recurrent or Resistant Neuroblastoma (IND#68,254) [NCT02075177] | 0 participants | Expanded Access | No longer available | ||||
| A Phase 1 Open-Label Study to Evaluate the Effect of CYP450 and P-gp Inhibition and Induction on the Pharmacokinetics of Pomalidomide (CC-4047) in Healthy Male Subjects [NCT01707407] | Phase 1 | 32 participants (Actual) | Interventional | 2012-09-01 | Completed | ||
| Relative Bioavailability of a Single Oral Dose of BI 144807 (Oral Solution) When Administered Alone or in Combination With Multiple Oral Doses of Ketoconazole (200 mg Tablet) in Healthy Male Subjects (an Open-label, Two-period, Fixed-sequence Trial) [NCT01707940] | Phase 1 | 24 participants (Actual) | Interventional | 2012-10-31 | Completed | ||
| An Open-label, Fixed-sequence, Single-centre Phase I Study to Assess the Effect of Ketoconazole on the Pharmacokinetics of AZD5069 After Oral Administration of a Single Dose AZD5069 to Healthy Male Volunteers [NCT01735240] | Phase 1 | 15 participants (Actual) | Interventional | 2012-12-31 | Completed | ||
| A Phase 1, Open Label Study In Healthy Subjects To Estimate The Effect Of Food And The Drug-Drug Interaction Potential Of Ketoconazole On PF-04449913 Pharmacokinetics [NCT01749085] | Phase 1 | 14 participants (Actual) | Interventional | 2012-12-31 | Completed | ||
| Identification and Evaluation of Endogenous Markers for the Assessment of CYP3A Activity in Female Subjects Using Metabolomics [NCT01760642] | Phase 1 | 16 participants (Actual) | Interventional | 2012-12-31 | Completed | ||
| A Phase I, Open-Label, Multicenter, Three-Period, One-Sequence Study To Investigate The Effect Of Ketoconazole On The Pharmacokinetics Of A Single Oral Dose Of 960 Mg Of Vemurafenib [NCT01765556] | Phase 1 | 0 participants (Actual) | Interventional | 2013-10-31 | Withdrawn | ||
| An Open Label Study in Healthy Volunteers to Investigate the Effect of Ketoconazole on the Pharmacokinetics of GSK239512 [NCT01802931] | Phase 1 | 22 participants (Actual) | Interventional | 2013-01-07 | Completed | ||
| Neoadjuvant Androgen Deprivation Therapy and Chemotherapy Followed by Radical Prostatectomy in Patients With Prostate Cancer [NCT02494713] | Phase 2 | 4 participants (Actual) | Interventional | 2015-10-31 | Terminated(stopped due to slow enrollment; resource re-allocation) | ||
| The Effect of Ketoconazole on Breathlessness During Resistive Load Breathing in Patients With Chronic Obstructive Pulmonary Disease [NCT01378520] | Phase 4 | 20 participants (Actual) | Interventional | 2011-06-30 | Completed | ||
| Effects of Potent Inhibition of CYP2C8, CYP2J2, and CYP3A4, Using Gemfibrozil, Ketoconazole, and Clarithromycin as Probes, on the Pharmacokinetics of LY2409021 in Healthy Subjects [NCT01836198] | Phase 1 | 30 participants (Actual) | Interventional | 2013-05-31 | Completed | ||
| Neuro-pharmacological Study of Ketoconazole for High-grade Gliomas: A Phase 0 Clinical Trial [NCT04869449] | Early Phase 1 | 5 participants (Anticipated) | Interventional | 2022-05-12 | Recruiting | ||
| A Phase I, Open-label, Randomised, Crossover Study in 3 Parallel Groups to Evaluate the Effect of Rifampicin, Ketoconazole, and Omeprazole on the Pharmacokinetics of Sativex in Healthy Volunteers [NCT01323465] | Phase 1 | 36 participants (Actual) | Interventional | 2008-02-29 | Completed | ||
| A Phase I, Open-Label, Fixed Sequence Study To Estimate The Steady-State Effect Of Ketoconazole On The Single-Dose Pharmacokinetics Of PF-04937319 In Healthy Adult Subjects [NCT01468714] | Phase 1 | 10 participants (Actual) | Interventional | 2011-10-31 | Completed | ||
| Relative Bioavailability of 10 mcg Olodaterol (Solution for Inhalation Administered With the Respimat) at Steady State Alone or in Combination With Multiple Doses of 400 mg q.d. Ketoconazole (Tablet) in Healthy Male and Female Volunteers (an Open Label, F [NCT01153711] | Phase 1 | 32 participants (Actual) | Interventional | 2010-05-31 | Completed | ||
| Seborrheic Dermatitis of the Scalp in Populations Practicing Less Frequent Hair Washing: Ketoconazole 2% Foam Versus Ketoconazole 2% Shampoo [NCT01203189] | 23 participants (Actual) | Interventional | 2010-09-30 | Completed | |||
| Utilizing Pharmacogenetics to Predict Drug Interactions in Kidney Transplant Recipients [NCT01288521] | Phase 4 | 8 participants (Actual) | Interventional | 2008-10-31 | Completed | ||
| An Open-Label, Two-Period, Fixed-Sequence Study to Evaluate the Effect of Multiple Doses of Ketoconazole on the Single Dose Pharmacokinetics of CC-223 in Healthy Adult Male Subjects [NCT01896323] | Phase 1 | 14 participants (Actual) | Interventional | 2013-07-01 | Completed | ||
| A Randomized, Single-center, Open-label, One-sequence, Two-period Crossover Study in 3 Parts to Investigate the Effects of Multiple Doses of Ketoconazole (Part 1), Rifampicin (Part 2), and Ritonavir-boosted Atazanavir (Part 3) on the PK of a Single Dose o [NCT01591850] | Phase 1 | 51 participants (Actual) | Interventional | 2011-09-30 | Completed | ||
| Optimizing the Treatment of Toenail Onychomycosis Using a New Transdermal Patch Combined With Terbinafine and Ketoconazole Formulation [NCT01615913] | Phase 1 | 18 participants (Anticipated) | Interventional | 2012-04-30 | Recruiting | ||
| Hormonal Mechanisms of Sleep Restriction - Axis Study [NCT03142893] | Phase 1 | 80 participants (Anticipated) | Interventional | 2017-05-08 | Active, not recruiting | ||
| Mechanisms of Control of the Intratesticular Hormonal Milieu in Man [NCT01215292] | Phase 1/Phase 2 | 46 participants (Actual) | Interventional | 2011-01-31 | Completed | ||
| A Phase 1, Randomized, Multiple Dose, Double Blind, 5-way Crossover Study of the Electrocardiographic Effects of Bilastine in Healthy Adult Subjects [NCT00419783] | Phase 1 | 30 participants (Actual) | Interventional | 2006-08-31 | Completed | ||
| A Phase I Investigation of Carboxyamido-triazole (CAI) Modulated by Ketoconozole In Patients With Advanced Malignancies [NCT00003249] | Phase 1 | 30 participants (Actual) | Interventional | 1998-05-31 | Completed | ||
| Phase 2 Study of Androgen Deprivation Therapy (ADT) Plus Chemotherapy as Initial Treatment for Local Failures or Advanced Prostate Cancer [NCT02560051] | Phase 2 | 19 participants (Actual) | Interventional | 2015-11-30 | Terminated(stopped due to Slow accrual; resource re-allocation) | ||
| Double-Blinded, Placebo-Controlled Trial to Explore the Anti-Androgen, Ketoconazole, for Treating Patients With an Ongoing Epidermal Growth Factor Receptor (EGFR) Inhibitor-Induced Rash [NCT03471364] | Early Phase 1 | 80 participants (Anticipated) | Interventional | 2018-08-22 | Recruiting | ||
| Maximal Suppression of the Androgen Axis in Clinically Localized Prostate Cancer [NCT00298155] | Phase 2 | 35 participants (Actual) | Interventional | 2006-07-31 | Completed | ||
| A Phase 1, Fixed Sequence, Cross-Over Study To Estimate The Effect Of Multiple Doses Of Ketoconazole On The Single Dose Pharmacokinetics Of Crizotinib (PF-02341066) In Healthy Volunteers [NCT01149785] | Phase 1 | 15 participants (Actual) | Interventional | 2010-07-31 | Completed | ||
| A One-Directional, Open-Label Drug Interaction Study to Investigate the Effects of Multiple-Dose Ketoconazole on Single-Dose Pharmacokinetics of Colchicine in Healthy Volunteers [NCT00983216] | Phase 1 | 24 participants (Actual) | Interventional | 2008-07-31 | Completed | ||
| Influence of CYP3A Modulation on Buprenorphine Disposition and Clinical Effects [NCT01576575] | 21 participants (Actual) | Interventional | 2010-06-30 | Completed | |||
| An Open-label Study in Healthy Male Subjects to Assess the Effect of a Strong CYP3A4 Inhibitor, Ketoconazole, on the Pharmacokinetics of Refametinib [NCT01925638] | Phase 1 | 18 participants (Actual) | Interventional | 2013-09-30 | Completed | ||
| A Phase 3 Trial of Androgen Ablation Alone vs. Chemo/Hormonal Therapy as Initial Treatment of Unresectable/Metastatic Adenocarcinoma of the Prostate [NCT00002855] | Phase 3 | 306 participants (Actual) | Interventional | 1996-08-31 | Completed | ||
| An Open Label, 2-Period, Sequential Study to Determine the Impact of Multiple Doses of Ketoconazole on Single-Dose Pharmacokinetics of HCV-796 [NCT00384917] | Phase 1 | 24 participants | Interventional | 2006-08-31 | Completed | ||
| A Phase I Evaluation of the Effect of Ketoconazole on the Pharmacokinetics and Safety of Dihydroergotamine Mesylate (DHE) Delivered by Oral Inhalation (MAP0004) in Healthy Volunteers Compared to DHE Delivered Intravenously (DHE 45®) [NCT01468558] | Phase 1 | 24 participants (Actual) | Interventional | 2010-07-31 | Completed | ||
| IAP104 - Assessment of Pharmacokinetic Changes Following Concurrent Administration of Sufentanil NanoTab and Ketoconazole in Healthy Subjects [NCT01721070] | Phase 1 | 19 participants (Actual) | Interventional | 2012-11-30 | Completed | ||
| A Phase 1 Study of Oral IXAZOMIB (MLN9708) to Assess Relative Bioavailability, Food Effect, Drug-Drug Interaction With Ketoconazole, Clarithromycin or Rifampin; and Safety and Tolerability in Patients With Advanced Nonhematologic Malignancies or Lymphoma [NCT01454076] | Phase 1 | 112 participants (Actual) | Interventional | 2011-11-10 | Completed | ||
| An Open Label Randomized Two-way Crossover Study to Investigate the Effect of Ketoconazole Mediated CYP3A4 Inhibition on the Single Oral Dose Pharmacokinetics of Tamsulosin in Healthy Male Volunteers (CYP2D6 Extensive Metabolizers) [NCT02264171] | Phase 1 | 24 participants (Actual) | Interventional | 2008-04-30 | Completed | ||
| Relative Bioavailability of Nintedanib Given Alone and in Combination With Ketoconazole at Steady State in Healthy Male Volunteers (an Open-label, Randomised, Two-way Cross-over Clinical Phase I Study) [NCT01679613] | Phase 1 | 34 participants (Actual) | Interventional | 2012-09-30 | Completed | ||
| Hormonal Mechanisms of Sleep Restriction - Axis Study in Older Men and Postmenopausal Women [NCT04037605] | Early Phase 1 | 5 participants (Actual) | Interventional | 2020-02-09 | Active, not recruiting | ||
| Hormonal Mechanisms of Sleep Restriction [NCT02256865] | Early Phase 1 | 40 participants (Actual) | Interventional | 2014-10-31 | Completed | ||
| A Phase 1 Study to Evaluate the Safety and Tolerability of LY2484595 SDSD-PG Tablets and the Effect of CYP3A Inhibition by Ketoconazole on the Pharmacokinetics of LY2484595 in Healthy Subjects [NCT01448824] | Phase 1 | 82 participants (Actual) | Interventional | 2011-10-31 | Completed | ||
| Relative Bioavailability of Single Oral Dose of BI 113608 When Administered Alone or in Combination With Multiple Oral Doses of Ketoconazole or Voriconazole in Healthy Male Subjects (an Open-label, Randomised, Three-period Cross-over Trial) [NCT01787032] | Phase 1 | 20 participants (Actual) | Interventional | 2013-01-31 | Completed | ||
| The Effect of Ketoconazole or Fluconazole on the Pharmacokinetics of Baricitinib in Healthy Subjects [NCT01924299] | Phase 1 | 36 participants (Actual) | Interventional | 2013-08-31 | Completed | ||
| [information is prepared from clinicaltrials.gov, extracted Sep-2024] | |||||||